S1208 |
Doxorubicin (DOX) HCl
|
ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution. |
-
Cell Metab, 2024, S1550-4131(24)00371-1
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nucleic Acids Res, 2024, gkae811
|
|
S1225 |
Etoposide
|
Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis. |
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nucleic Acids Res, 2024, gkae316
-
Redox Biol, 2024, 76:103323
|
|
S1288 |
Camptothecin (CPT)
|
Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2. |
-
Nat Commun, 2024, 15(1):4430
-
Exp Mol Med, 2024, 56(3):656-673
-
Mol Oncol, 2024, 10.1002/1878-0261.13577
|
|
S2217 |
Irinotecan HCl Trihydrate
|
Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively. |
-
J Exp Clin Cancer Res, 2024, 43(1):151
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
-
Int Immunopharmacol, 2023, 119:110205
|
|
S4908 |
SN-38
|
SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy. |
-
Cell, 2024, 187(20):5698-5718.e26
-
Nat Commun, 2024, 15(1):2503
-
Cell Rep Med, 2024, 5(7):101627
|
|
S3035 |
Daunorubicin HCl
|
Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
-
Nat Commun, 2024, 15(1):4739
-
Haematologica, 2024, 109(6):1713-1725
-
Int J Oncol, 2024, 64(6)66
|
|
E2516 |
Doxorubicin
|
Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM. |
-
Nat Commun, 2024, 15(1):4450
-
Nat Commun, 2024, 15(1):1041
-
Theranostics, 2024, 14(9):3719-3738
|
|
S1228 |
Idarubicin HCl
|
Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy. |
-
Cell Rep, 2024, 43(7):114388
-
BMC Pharmacol Toxicol, 2024, 25(1):25
-
Mol Cell, 2023, 83(13):2206-2221.e11
|
|
S1231 |
Topotecan HCl
|
Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis. |
-
Mol Cell, 2024, 84(14):2618-2633.e10
-
Cancer Cell Int, 2024, 24(1):285
-
iScience, 2024, 27(1):108667
|
|
S2485 |
Mitoxantrone 2HCl
|
Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
-
Mol Metab, 2024, 80:101873
-
Blood Adv, 2024, 8(15):4017-4024
-
BMC Pharmacol Toxicol, 2024, 25(1):25
|
|
S1198 |
Irinotecan
|
Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
BMC Cancer, 2024, 24(1):357
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
|
|
S1223 |
Epirubicin HCl
|
Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis. |
-
Cell Death Dis, 2024, 15(7):480
-
Front Immunol, 2024, 15:1470328
-
Front Pharmacol, 2023, 14:1189245
|
|
S1342 |
Genistein
|
Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM. |
-
Int J Nanomedicine, 2023, 18:4647-4662
-
Molecules, 2023, 28(4)1919
-
Exp Ther Med, 2023, 26(5):516
|
|
S9321 |
Topotecan
|
Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. |
-
MedComm (2020), 2024, 5(8):e684
-
Cell Rep Med, 2023, 4(6):101091
-
Cell Rep Med, 2023, 4(6):101091
|
|
S5026 |
Irinotecan hydrochloride
|
Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
-
Drug Resist Updat, 2023, 71:101005
-
PLoS Biol, 2023, 21(9):e3002256
-
PLoS Biol, 2023, 21(9):e3002256
|
|
S1787 |
Teniposide
|
Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL). |
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
-
bioRxiv, 2023, 2023.01.17.524444
-
Cancers (Basel), 2022, 14(19)4883
|
|
S2492 |
Novobiocin Sodium (NSC 2382)
|
Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria. |
-
Cell Rep, 2024, 43(5):114205
-
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0292
-
Nat Commun, 2023, 14(1):1390
|
|
S3603 |
Betulinic acid
|
Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. It's reported that Betulinic acid acts as a new activator of NF-κB.Phase 1/2. |
-
World J Stem Cells, 2024, 16(5):575-590
-
J Orthop Surg Res, 2024, 19(1):188
-
Bioact Mater, 2023, 25:594-614
|
|
S1393 |
Pirarubicin
|
Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent. |
-
Cell Death Dis, 2022, 13(5):492
-
Int J Nanomedicine, 2021, 16:951-976
-
Pharmaceuticals (Basel), 2020, 14(1)E22
|
|
S7261 |
Beta-Lapachone
|
Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. |
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
-
Int J Oncol, 2023, 62(3)42
-
Comput Struct Biotechnol J, 2022, 20:2442-2454
|
|
S2423 |
(S)-10-Hydroxycamptothecin
|
(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity. |
-
Eur J Med Res, 2023, 28(1):326
-
Eur J Med Res, 2023, 28(1):326
-
Nat Commun, 2022, 13(1):2861
|
|
S1367 |
Amonafide
|
Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3. |
-
Viruses, 2022, 15(1)105
-
Nat Commun, 2019, 10(1):4217
-
Front Oncol, 2019, 9:1406
|
|
S1222 |
Dexrazoxane HCl
|
Dexrazoxane HCl is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II |
-
Adv Sci -Weinh), 2023, 10(30):e2301136
-
Adv Sci (Weinh), 2023, 10(30):e2301136
-
Sci Adv, 2023, 9(49):eadi6681
|
|
S1940 |
Levofloxacin
|
Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections. |
-
Adv Healthc Mater, 2022, e2102117
-
Exp Ther Med, 2021, 21(4):332
-
Mol Cell, 2020, 80(6):1104-1122.e9
|
|
S7518 |
Voreloxin (SNS-595) hydrochloride
|
Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2. |
-
Viruses, 2022, 15(1)105
-
Adv Sci (Weinh), 2020, 7(21):2001018
-
Apoptosis, 2019, 24(11-12):849-861
|
|
S1465 |
Moxifloxacin (BAY12-8039) HCl
|
Moxifloxacin (Avelox, Avalox,BAY12-8039 HCl) is a fourth-generation synthetic fluoroquinolone antibacterial agent. |
-
Microorganisms, 2022, 10(7)1421
-
Clin Transl Sci, 2019, 12(6):687-697
-
Front Microbiol, 2018, 6:336
|
|
S1327 |
Ellagic acid
|
Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property. |
-
J Ethnopharmacol, 2024, 330:118227
-
Mol Cell, 2020, 80(6):1104-1122.e9
-
Kaohsiung J Med Sci, 2020, 6
|
|
S1756 |
Enoxacin
|
Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections. |
-
Cell Death Discov, 2023, 9(1):21
-
Cell Death Discov, 2023, 9(1):173
-
J Virol, 2022, 96(15):e0187421
|
|
S4604 |
Levofloxacin hydrate
|
Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II). |
-
Adv Healthc Mater, 2022, e2102117
-
Exp Ther Med, 2021, 21(4):332
-
Front Microbiol, 2020, 10:2936
|
|
S1340 |
Gatifloxacin
|
Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. |
-
Cancer Discov, 2020, CD-20-0160
-
Biochem Pharmacol, 2015, 95(4):227-37
|
|
S2027 |
Ciprofloxacin
|
Ciprofloxacin (Bay o 9867,Bay q 3939) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM. |
-
Nanomaterials (Basel), 2021, 11(8)1984
-
Environ Mol Mutagen, 2019, 60(6):513-533
|
|
S2328 |
Nalidixic acid
|
Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase. |
-
Hum Mol Genet, 2020, ddaa244
-
Int J Mol Sci, 2018, 19(6)
|
|
S5059 |
Pixantrone Maleate
|
Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites. |
-
Eur J Pharmacol, 2024, 979:176835
-
Genes Dev, 2023, 37(17-18):844-860
-
bioRxiv, 2023, 2023.05.25.542379
|
|
S1463 |
Ofloxacin
|
Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent. |
-
Molecules, 2023, 28(3)1444
|
|
S5008 |
Ciprofloxacin (CPX) hydrochloride
|
Ciprofloxacin (CPX) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases). |
-
Nanomaterials (Basel), 2021, 11(8)1984
|
|
S0093 |
Genz-644282
|
Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.The solubility of this product is not good, please choose carefully for cell experiments! |
-
Commun Biol, 2022, 5(1):982
|
|
S6790 |
Ellipticine hydrochloride
|
Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity. |
-
Viruses, 2022, 15(1)105
|
|
S9634 |
Phenoxodiol (Haginin E)
|
Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II. |
-
Anticancer Res, 2018, 38(10):5709-5716
|
|
S3898 |
Hydroxy Camptothecine
|
Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. |
-
Life Sci, 2020, 246:117428
|
|
S2288 |
Rubitecan
|
Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity. |
-
Chem Biol Drug Des, 2022, 100(5):699-721
|
|
S1464 |
Marbofloxacin
|
Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication. |
|
|
S1509 |
Norfloxacin
|
Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes. |
-
J Chromatogr A, 2024, 1734:465286
|
|
S4006 |
Clinafloxacin
|
Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. |
|
|
S6747 |
SW-044248
|
SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. |
|
|
E4801New |
Cu(II)-Elesclomol
|
Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity. |
-
Leukemia, 2024, 10.1038/s41375-024-02442-0
|
|
S4119 |
Pefloxacin Mesylate Dihydrate
|
Pefloxacin Mesylate Dihydrate (1589 RB,Pefloxacinium mesylate dihydrate) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication. |
|
|
S5627 |
Amsacrine hydrochloride
|
Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity. |
|
|
S5964 |
Gatifloxacin hydrochloride
|
Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively. |
|
|
S2064 |
Balofloxacin
|
Balofloxacin (Q-35,Q-roxin) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase. |
|
|
E1905New |
Nalidixic acid sodium salt
|
Nalidixic acid sodium salt is an inhibitor of bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA supercoiling during replication, making it an effective quinolone antibiotic against both gram-positive and gram-negative bacteria. |
|
|
S8942 |
Suramin sodium salt
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). |
-
J Biol Chem, 2024, S0021-9258(24)00128-5
|
|
S2271 |
Berberine chloride
|
Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
-
Adv Healthc Mater, 2023, e2300591.
-
Transl Oncol, 2023, 35:101712
-
J Biomol Struct Dyn, 2022, 1-11
|
|
E4811New |
Levofloxacin hydrochloride
|
Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. |
|
|
E2891 |
Dxd
|
Dxd(Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM. |
|
|
S5111 |
7-Ethylcamptothecin
|
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. |
|
|
S2653 |
9-amino-CPT (9-Aminocamptothecin)
|
9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin. |
|
|
E4925New |
Amsacrine
|
Amsacrine(m-AMSA, acridinyl anisidide) is an inhibitor of topoisomerase II. Amsacrine acts as an antineoplastic agent which intercalates into the DNA of tumor cells, it is also used in the treatment of acute myelogenous leukemia. |
|
|
S6631 |
Belotecan (CKD-602) hydrochloride
|
Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. |
|
|
S3181 |
Flumequine
|
Flumequine(R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
|
|
E1769New |
Merbarone
|
Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. |
|
|
S8999 |
Exatecan Mesylate
|
Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml. |
|
|
S1208 |
Doxorubicin (DOX) HCl
|
ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution. |
- Cell Metab, 2024, S1550-4131(24)00371-1
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nucleic Acids Res, 2024, gkae811
|
|
S1225 |
Etoposide
|
Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis. |
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nucleic Acids Res, 2024, gkae316
- Redox Biol, 2024, 76:103323
|
|
S1288 |
Camptothecin (CPT)
|
Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2. |
- Nat Commun, 2024, 15(1):4430
- Exp Mol Med, 2024, 56(3):656-673
- Mol Oncol, 2024, 10.1002/1878-0261.13577
|
|
S2217 |
Irinotecan HCl Trihydrate
|
Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively. |
- J Exp Clin Cancer Res, 2024, 43(1):151
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
- Int Immunopharmacol, 2023, 119:110205
|
|
S4908 |
SN-38
|
SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy. |
- Cell, 2024, 187(20):5698-5718.e26
- Nat Commun, 2024, 15(1):2503
- Cell Rep Med, 2024, 5(7):101627
|
|
S3035 |
Daunorubicin HCl
|
Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
- Nat Commun, 2024, 15(1):4739
- Haematologica, 2024, 109(6):1713-1725
- Int J Oncol, 2024, 64(6)66
|
|
E2516 |
Doxorubicin
|
Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM. |
- Nat Commun, 2024, 15(1):4450
- Nat Commun, 2024, 15(1):1041
- Theranostics, 2024, 14(9):3719-3738
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S1228 |
Idarubicin HCl
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Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy. |
- Cell Rep, 2024, 43(7):114388
- BMC Pharmacol Toxicol, 2024, 25(1):25
- Mol Cell, 2023, 83(13):2206-2221.e11
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S1231 |
Topotecan HCl
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Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis. |
- Mol Cell, 2024, 84(14):2618-2633.e10
- Cancer Cell Int, 2024, 24(1):285
- iScience, 2024, 27(1):108667
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S2485 |
Mitoxantrone 2HCl
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Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
- Mol Metab, 2024, 80:101873
- Blood Adv, 2024, 8(15):4017-4024
- BMC Pharmacol Toxicol, 2024, 25(1):25
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S1198 |
Irinotecan
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Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- BMC Cancer, 2024, 24(1):357
- Environ Mol Mutagen, 2024, 10.1002/em.22604
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S1223 |
Epirubicin HCl
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Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis. |
- Cell Death Dis, 2024, 15(7):480
- Front Immunol, 2024, 15:1470328
- Front Pharmacol, 2023, 14:1189245
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S1342 |
Genistein
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Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM. |
- Int J Nanomedicine, 2023, 18:4647-4662
- Molecules, 2023, 28(4)1919
- Exp Ther Med, 2023, 26(5):516
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S9321 |
Topotecan
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Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. |
- MedComm (2020), 2024, 5(8):e684
- Cell Rep Med, 2023, 4(6):101091
- Cell Rep Med, 2023, 4(6):101091
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S5026 |
Irinotecan hydrochloride
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Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
- Drug Resist Updat, 2023, 71:101005
- PLoS Biol, 2023, 21(9):e3002256
- PLoS Biol, 2023, 21(9):e3002256
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S1787 |
Teniposide
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Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL). |
- Environ Mol Mutagen, 2024, 10.1002/em.22604
- bioRxiv, 2023, 2023.01.17.524444
- Cancers (Basel), 2022, 14(19)4883
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S2492 |
Novobiocin Sodium (NSC 2382)
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Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria. |
- Cell Rep, 2024, 43(5):114205
- Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0292
- Nat Commun, 2023, 14(1):1390
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S3603 |
Betulinic acid
|
Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. It's reported that Betulinic acid acts as a new activator of NF-κB.Phase 1/2. |
- World J Stem Cells, 2024, 16(5):575-590
- J Orthop Surg Res, 2024, 19(1):188
- Bioact Mater, 2023, 25:594-614
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S1393 |
Pirarubicin
|
Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent. |
- Cell Death Dis, 2022, 13(5):492
- Int J Nanomedicine, 2021, 16:951-976
- Pharmaceuticals (Basel), 2020, 14(1)E22
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S7261 |
Beta-Lapachone
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Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. |
- Environ Mol Mutagen, 2024, 10.1002/em.22604
- Int J Oncol, 2023, 62(3)42
- Comput Struct Biotechnol J, 2022, 20:2442-2454
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S2423 |
(S)-10-Hydroxycamptothecin
|
(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity. |
- Eur J Med Res, 2023, 28(1):326
- Eur J Med Res, 2023, 28(1):326
- Nat Commun, 2022, 13(1):2861
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S1367 |
Amonafide
|
Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3. |
- Viruses, 2022, 15(1)105
- Nat Commun, 2019, 10(1):4217
- Front Oncol, 2019, 9:1406
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S1222 |
Dexrazoxane HCl
|
Dexrazoxane HCl is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II |
- Adv Sci -Weinh), 2023, 10(30):e2301136
- Adv Sci (Weinh), 2023, 10(30):e2301136
- Sci Adv, 2023, 9(49):eadi6681
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S1940 |
Levofloxacin
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Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections. |
- Adv Healthc Mater, 2022, e2102117
- Exp Ther Med, 2021, 21(4):332
- Mol Cell, 2020, 80(6):1104-1122.e9
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S7518 |
Voreloxin (SNS-595) hydrochloride
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Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2. |
- Viruses, 2022, 15(1)105
- Adv Sci (Weinh), 2020, 7(21):2001018
- Apoptosis, 2019, 24(11-12):849-861
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S1465 |
Moxifloxacin (BAY12-8039) HCl
|
Moxifloxacin (Avelox, Avalox,BAY12-8039 HCl) is a fourth-generation synthetic fluoroquinolone antibacterial agent. |
- Microorganisms, 2022, 10(7)1421
- Clin Transl Sci, 2019, 12(6):687-697
- Front Microbiol, 2018, 6:336
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S1327 |
Ellagic acid
|
Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property. |
- J Ethnopharmacol, 2024, 330:118227
- Mol Cell, 2020, 80(6):1104-1122.e9
- Kaohsiung J Med Sci, 2020, 6
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S1756 |
Enoxacin
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Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections. |
- Cell Death Discov, 2023, 9(1):21
- Cell Death Discov, 2023, 9(1):173
- J Virol, 2022, 96(15):e0187421
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S4604 |
Levofloxacin hydrate
|
Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II). |
- Adv Healthc Mater, 2022, e2102117
- Exp Ther Med, 2021, 21(4):332
- Front Microbiol, 2020, 10:2936
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S1340 |
Gatifloxacin
|
Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. |
- Cancer Discov, 2020, CD-20-0160
- Biochem Pharmacol, 2015, 95(4):227-37
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S2027 |
Ciprofloxacin
|
Ciprofloxacin (Bay o 9867,Bay q 3939) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM. |
- Nanomaterials (Basel), 2021, 11(8)1984
- Environ Mol Mutagen, 2019, 60(6):513-533
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S2328 |
Nalidixic acid
|
Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase. |
- Hum Mol Genet, 2020, ddaa244
- Int J Mol Sci, 2018, 19(6)
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S5059 |
Pixantrone Maleate
|
Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites. |
- Eur J Pharmacol, 2024, 979:176835
- Genes Dev, 2023, 37(17-18):844-860
- bioRxiv, 2023, 2023.05.25.542379
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S1463 |
Ofloxacin
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Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent. |
- Molecules, 2023, 28(3)1444
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S5008 |
Ciprofloxacin (CPX) hydrochloride
|
Ciprofloxacin (CPX) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases). |
- Nanomaterials (Basel), 2021, 11(8)1984
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S0093 |
Genz-644282
|
Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.The solubility of this product is not good, please choose carefully for cell experiments! |
- Commun Biol, 2022, 5(1):982
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S6790 |
Ellipticine hydrochloride
|
Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity. |
- Viruses, 2022, 15(1)105
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S3898 |
Hydroxy Camptothecine
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Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. |
- Life Sci, 2020, 246:117428
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S2288 |
Rubitecan
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Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity. |
- Chem Biol Drug Des, 2022, 100(5):699-721
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S1464 |
Marbofloxacin
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Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication. |
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S1509 |
Norfloxacin
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Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes. |
- J Chromatogr A, 2024, 1734:465286
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S4006 |
Clinafloxacin
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Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. |
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S6747 |
SW-044248
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SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. |
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E4801New |
Cu(II)-Elesclomol
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Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity. |
- Leukemia, 2024, 10.1038/s41375-024-02442-0
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S4119 |
Pefloxacin Mesylate Dihydrate
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Pefloxacin Mesylate Dihydrate (1589 RB,Pefloxacinium mesylate dihydrate) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication. |
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S5627 |
Amsacrine hydrochloride
|
Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity. |
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S5964 |
Gatifloxacin hydrochloride
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Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively. |
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S2064 |
Balofloxacin
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Balofloxacin (Q-35,Q-roxin) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase. |
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E1905New |
Nalidixic acid sodium salt
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Nalidixic acid sodium salt is an inhibitor of bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA supercoiling during replication, making it an effective quinolone antibiotic against both gram-positive and gram-negative bacteria. |
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S8942 |
Suramin sodium salt
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Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). |
- J Biol Chem, 2024, S0021-9258(24)00128-5
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S2271 |
Berberine chloride
|
Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
- Adv Healthc Mater, 2023, e2300591.
- Transl Oncol, 2023, 35:101712
- J Biomol Struct Dyn, 2022, 1-11
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E4811New |
Levofloxacin hydrochloride
|
Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. |
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E2891 |
Dxd
|
Dxd(Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM. |
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S5111 |
7-Ethylcamptothecin
|
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. |
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S2653 |
9-amino-CPT (9-Aminocamptothecin)
|
9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin. |
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E4925New |
Amsacrine
|
Amsacrine(m-AMSA, acridinyl anisidide) is an inhibitor of topoisomerase II. Amsacrine acts as an antineoplastic agent which intercalates into the DNA of tumor cells, it is also used in the treatment of acute myelogenous leukemia. |
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S6631 |
Belotecan (CKD-602) hydrochloride
|
Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. |
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S3181 |
Flumequine
|
Flumequine(R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
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E1769New |
Merbarone
|
Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. |
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S8999 |
Exatecan Mesylate
|
Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml. |
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