S1060 |
Olaparib (AZD2281)
|
オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。 |
-
Nature, 2024, 10.1038/s41586-024-07217-2
-
Nature, 2024, 628(8007):433-441
-
Cell, 2024, 187(4):945-961.e18
|
|
S1180 |
XAV-939
|
XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
-
Adv Sci (Weinh), 2024, 11(1):e2303637
-
J Nanobiotechnology, 2024, 22(1):373
-
Cell Death Dis, 2024, 15(3):211
|
|
S1004 |
Veliparib (ABT-888)
|
Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3. |
-
Nature, 2024, 10.1038/s41586-024-07217-2
-
Nature, 2024, 628(8007):433-441
-
Cell Rep, 2024, 43(5):114205
|
|
S7048 |
Talazoparib (BMN 673)
|
タラゾパリブ (Talazoparib (BMN 673、LT-673)) は、新規 PARP 阻害剤 (無細胞アッセイで IC50 = 0.57 nM) です。 また PARP-2 の強力な阻害剤でもありますが、PARG を阻害せず PTEN 変異に非常に敏感です。 臨床フェーズ 3。 |
-
Nature, 2024, 10.1038/s41586-024-07217-2
-
Nature, 2024, 628(8007):433-441
-
Gastroenterology, 2024, S0016-5085(24)00062-3
|
|
S1098 |
Rucaparib phosphate
|
Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
-
Int J Mol Sci, 2024, 25(2)886
-
J Biol Chem, 2024, 300(6):107377
-
Cancer Res, 2023, 83(10):1699-1710
|
|
S2741 |
Niraparib (MK-4827)
|
ニラパリブ (Niraparib (MK-4827)) は PARP1/2 の選択的阻害剤 (IC50 = 3.8 nM/2.1 nM) であり、変異型 BRCA-1 および BRCA-2 を持つ癌細胞で高い活性を示します。PARP3, V-PARP, Tank1 に比べて 330 倍以上の選択性があります。 ニラパリブは PARP-DNA 複合体を形成し、DNA損傷、アポトーシス (apoptossis)、および細胞死を引き起こします。臨床フェーズ 3。 |
-
Nat Genet, 2024, 10.1038/s41588-024-01948-8
-
EBioMedicine, 2024, 103:105129
-
Cell Death Discov, 2024, 10(1):74
|
|
S7300 |
PJ34 HCl
|
PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
-
J Neuroinflammation, 2024, 21(1):235
-
Nat Commun, 2023, 14(1):7161
-
Nat Commun, 2023, 14(1):4310
|
|
S4948 |
Rucaparib
|
Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
-
Nat Commun, 2024, 15(1):2862
-
Nucleic Acids Res, 2024, gkae316
-
EBioMedicine, 2024, 103:105129
|
|
S7625 |
Niraparib tosylate
|
Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
-
Nat Commun, 2024, 15(1):1041
-
Cancer Res, 2023, 83(10):1699-1710
-
Cancer Res, 2023, 83(16):2750-2762
|
|
S2178 |
AG-14361
|
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
-
Nat Commun, 2024, 15(1):1041
-
Cell Stem Cell, 2022, S1934-5909(22)00010-8
-
Cell Rep, 2022, 39(12):110994
|
|
S1087 |
Iniparib (BSI-201)
|
Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
-
Nat Commun, 2021, 12(1):736
-
Front Oncol, 2021, 11:773186
-
PLoS Pathog, 2020, 21;16(4):e1008474
|
|
S5195 |
Rucaparib Camsylate
|
Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
-
Adv Sci (Weinh), 2022, 9(30):e2201210
-
Cell Death Dis, 2022, 13(6):558
-
Int J Mol Sci, 2022, 23(10)5770
|
|
S2197 |
A-966492
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
-
Nat Commun, 2021, 12(1):736
-
Front Immunol, 2021, 12:712021
-
Front Immunol, 2021, 12:712021
|
|
S7239 |
G007-LK
|
G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
|
-
EBioMedicine, 2024, 103:105129
-
bioRxiv, 2024, 2024.02.02.578667
-
Nat Commun, 2023, 14(1):110
|
|
S8038 |
UPF 1069
|
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
-
Cell Rep, 2023, 42(9):113113
-
Res Sq, 2023, rs.3.rs-2688694
-
Res Sq, 2023, rs.3.rs-2688694
|
|
S7029 |
AZD2461
|
AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1. |
-
Nat Commun, 2021, 12(1):736
-
Cell Chem Biol, 2021, S2451-9456(21)00058-1
-
Dev Cell, 2020, 53(2):240-252.e7
|
|
S8592 |
Pamiparib
|
Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
-
Cell Death Discov, 2024, 10(1):74
-
Clin Cancer Res, 2023, 29(9):1763-1782
-
J Neurooncol, 2023, 164(3):617-632
|
|
S1132 |
3-Aminobenzamide
|
3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
-
Int J Mol Sci, 2023, 24(2)1667
-
Psychopharmacology (Berl), 2022, 10.1007/s00213-022-06188-4
-
Cell Death Discov, 2021, 7(1):181
|
|
S7438 |
ME0328
|
ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
-
Biomed Pharmacother, 2018, 97:115-119
-
Mol Cancer Ther, 2018, 17(10):2206-2216
-
Breast Cancer Res Treat, 2018, 172(1):23-32
|
|
S8363 |
NMS-P118
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
-
Res Sq, 2023, rs.3.rs-2688694
-
Res Sq, 2023, rs.3.rs-2688694
-
Int J Biol Sci, 2022, 18(3):1238-1253
|
|
S8419 |
Stenoparib (E7449)
|
Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
-
Br J Pharmacol, 2024, 10.1111/bph.17305
-
Cell Death Discov, 2024, 10(1):74
-
J Cell Mol Med, 2024, 28(12):e18467
|
|
S7238 |
NVP-TNKS656
|
NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
|
-
Cell, 2024, 187(14):3671-3689.e23
-
bioRxiv, 2023, 2023.07.19.549714
-
bioRxiv, 2023, 2023.07.19.549714
|
|
S7490 |
WIKI4
|
WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
|
-
Sci Rep, 2022, 12(1):7
-
Carcinogenesis, 2020, 41(7):993-1004
-
Nat Commun, 2019, 10(1):4363
|
|
S4715 |
Benzamide
|
Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid. |
-
Int J Mol Sci, 2019, 20(21)
-
Mol Pharmacol, 2019, 96(4):419-429
-
Acta Neuropathol Commun, 2014, 2:57
|
|
S8370 |
BGP-15 2HCl
|
BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
-
Part Fibre Toxicol, 2023, 20(1):28
-
Part Fibre Toxicol, 2023, 20(1):28
-
Respir Res, 2023, 24(1):319
|
|
S7730 |
NU1025
|
NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
|
-
J Clin Med, 2020, 30;9(4)
-
Med Sci Monit, 2019, 25:2886-2895
|
|
S5967 |
Berberine chloride hydrate
|
Berberine (Natural Yellow 18) chloride hydrate 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. |
-
Front Biosci (Landmark Ed), 2022, 27(8):242
-
Front Pharmacol, 2021, 12:632201
|
|
S6745 |
JW55
|
JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
-
Cell Discov, 2024, 10(1):39
-
Oncotarget, 2021, 12(7):674-685
-
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
|
|
S0519 |
BYK204165
|
BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
-
Sci Transl Med, 2021, 13(592)eabc7211
|
|
S9712 |
Fluzoparib (SHR-3162)
|
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity with an IC50 of 1.46±0.72 nM for PARP1. |
-
Biochemistry, 2023, 62(16):2382-2390
|
|
S4710 |
Picolinamide
|
Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
-
Neural Regen Res, 2023, 18(10):2252-2259
-
Neural Regen Res, 2023, 18(10):2252-2259
|
|
E1425 |
Nesuparib
|
Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. Nesuparib exhibits anti-tumor activity in BRCA-deficient xenograft models. |
|
|
S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
|
|
S6977 |
DR2313
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. |
|
|
S6739 |
MN 64
|
MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. |
|
|
S0913 |
4',5,7-Trimethoxyflavone
|
4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein. |
|
|
E1069 |
M2912
|
M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity. |
|
|
S0732 |
GeA-69
|
GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. |
|
|
S8993 |
Atamparib (RBN-2397)
|
Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment. |
-
bioRxiv, 2024, 2024.03.15.584457
|
|
E1614New |
OUL232
|
OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies. |
|
|
S9893 |
Venadaparib(IDX-1197)
|
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. |
|
|
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
|
|
S6882 |
HI-TOPK-032
|
HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. |
|
|
E4869New |
Niraparib hydrochloride
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity. |
|
|
S9360 |
4-Hydroxyquinazoline
|
4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. |
|
|
S8992 |
RBN012759
|
RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response. |
|
|
S9875 |
Saruparib (AZD5305)
|
Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).
|
-
Nature, 2024, 10.1038/s41586-024-07217-2
-
Nature, 2024, 628(8007):433-441
-
Nat Commun, 2024, 15(1):5822
|
|
E2147 |
AZD9574
|
AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule. |
|
|
S8876 |
RK-287107
|
RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. |
|
|
S1060 |
Olaparib (AZD2281)
|
オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。 |
- Nature, 2024, 10.1038/s41586-024-07217-2
- Nature, 2024, 628(8007):433-441
- Cell, 2024, 187(4):945-961.e18
|
|
S1180 |
XAV-939
|
XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
- Adv Sci (Weinh), 2024, 11(1):e2303637
- J Nanobiotechnology, 2024, 22(1):373
- Cell Death Dis, 2024, 15(3):211
|
|
S1004 |
Veliparib (ABT-888)
|
Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3. |
- Nature, 2024, 10.1038/s41586-024-07217-2
- Nature, 2024, 628(8007):433-441
- Cell Rep, 2024, 43(5):114205
|
|
S7048 |
Talazoparib (BMN 673)
|
タラゾパリブ (Talazoparib (BMN 673、LT-673)) は、新規 PARP 阻害剤 (無細胞アッセイで IC50 = 0.57 nM) です。 また PARP-2 の強力な阻害剤でもありますが、PARG を阻害せず PTEN 変異に非常に敏感です。 臨床フェーズ 3。 |
- Nature, 2024, 10.1038/s41586-024-07217-2
- Nature, 2024, 628(8007):433-441
- Gastroenterology, 2024, S0016-5085(24)00062-3
|
|
S1098 |
Rucaparib phosphate
|
Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
- Int J Mol Sci, 2024, 25(2)886
- J Biol Chem, 2024, 300(6):107377
- Cancer Res, 2023, 83(10):1699-1710
|
|
S2741 |
Niraparib (MK-4827)
|
ニラパリブ (Niraparib (MK-4827)) は PARP1/2 の選択的阻害剤 (IC50 = 3.8 nM/2.1 nM) であり、変異型 BRCA-1 および BRCA-2 を持つ癌細胞で高い活性を示します。PARP3, V-PARP, Tank1 に比べて 330 倍以上の選択性があります。 ニラパリブは PARP-DNA 複合体を形成し、DNA損傷、アポトーシス (apoptossis)、および細胞死を引き起こします。臨床フェーズ 3。 |
- Nat Genet, 2024, 10.1038/s41588-024-01948-8
- EBioMedicine, 2024, 103:105129
- Cell Death Discov, 2024, 10(1):74
|
|
S7300 |
PJ34 HCl
|
PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
- J Neuroinflammation, 2024, 21(1):235
- Nat Commun, 2023, 14(1):7161
- Nat Commun, 2023, 14(1):4310
|
|
S4948 |
Rucaparib
|
Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
- Nat Commun, 2024, 15(1):2862
- Nucleic Acids Res, 2024, gkae316
- EBioMedicine, 2024, 103:105129
|
|
S7625 |
Niraparib tosylate
|
Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
- Nat Commun, 2024, 15(1):1041
- Cancer Res, 2023, 83(10):1699-1710
- Cancer Res, 2023, 83(16):2750-2762
|
|
S2178 |
AG-14361
|
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
- Nat Commun, 2024, 15(1):1041
- Cell Stem Cell, 2022, S1934-5909(22)00010-8
- Cell Rep, 2022, 39(12):110994
|
|
S1087 |
Iniparib (BSI-201)
|
Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
- Nat Commun, 2021, 12(1):736
- Front Oncol, 2021, 11:773186
- PLoS Pathog, 2020, 21;16(4):e1008474
|
|
S5195 |
Rucaparib Camsylate
|
Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
- Adv Sci (Weinh), 2022, 9(30):e2201210
- Cell Death Dis, 2022, 13(6):558
- Int J Mol Sci, 2022, 23(10)5770
|
|
S2197 |
A-966492
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
- Nat Commun, 2021, 12(1):736
- Front Immunol, 2021, 12:712021
- Front Immunol, 2021, 12:712021
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S7239 |
G007-LK
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G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
|
- EBioMedicine, 2024, 103:105129
- bioRxiv, 2024, 2024.02.02.578667
- Nat Commun, 2023, 14(1):110
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S8038 |
UPF 1069
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UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
- Cell Rep, 2023, 42(9):113113
- Res Sq, 2023, rs.3.rs-2688694
- Res Sq, 2023, rs.3.rs-2688694
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S7029 |
AZD2461
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AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1. |
- Nat Commun, 2021, 12(1):736
- Cell Chem Biol, 2021, S2451-9456(21)00058-1
- Dev Cell, 2020, 53(2):240-252.e7
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S8592 |
Pamiparib
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Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
- Cell Death Discov, 2024, 10(1):74
- Clin Cancer Res, 2023, 29(9):1763-1782
- J Neurooncol, 2023, 164(3):617-632
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S1132 |
3-Aminobenzamide
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3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
- Int J Mol Sci, 2023, 24(2)1667
- Psychopharmacology (Berl), 2022, 10.1007/s00213-022-06188-4
- Cell Death Discov, 2021, 7(1):181
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S7438 |
ME0328
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ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
- Biomed Pharmacother, 2018, 97:115-119
- Mol Cancer Ther, 2018, 17(10):2206-2216
- Breast Cancer Res Treat, 2018, 172(1):23-32
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S8363 |
NMS-P118
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NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
- Res Sq, 2023, rs.3.rs-2688694
- Res Sq, 2023, rs.3.rs-2688694
- Int J Biol Sci, 2022, 18(3):1238-1253
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S8419 |
Stenoparib (E7449)
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Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
- Br J Pharmacol, 2024, 10.1111/bph.17305
- Cell Death Discov, 2024, 10(1):74
- J Cell Mol Med, 2024, 28(12):e18467
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S7238 |
NVP-TNKS656
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NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
|
- Cell, 2024, 187(14):3671-3689.e23
- bioRxiv, 2023, 2023.07.19.549714
- bioRxiv, 2023, 2023.07.19.549714
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S7490 |
WIKI4
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WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
|
- Sci Rep, 2022, 12(1):7
- Carcinogenesis, 2020, 41(7):993-1004
- Nat Commun, 2019, 10(1):4363
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S4715 |
Benzamide
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Benzamide, an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid. |
- Int J Mol Sci, 2019, 20(21)
- Mol Pharmacol, 2019, 96(4):419-429
- Acta Neuropathol Commun, 2014, 2:57
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S8370 |
BGP-15 2HCl
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BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
- Part Fibre Toxicol, 2023, 20(1):28
- Part Fibre Toxicol, 2023, 20(1):28
- Respir Res, 2023, 24(1):319
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S7730 |
NU1025
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NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
|
- J Clin Med, 2020, 30;9(4)
- Med Sci Monit, 2019, 25:2886-2895
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S6745 |
JW55
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JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
- Cell Discov, 2024, 10(1):39
- Oncotarget, 2021, 12(7):674-685
- Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
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S0519 |
BYK204165
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BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
- Sci Transl Med, 2021, 13(592)eabc7211
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S9712 |
Fluzoparib (SHR-3162)
|
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity with an IC50 of 1.46±0.72 nM for PARP1. |
- Biochemistry, 2023, 62(16):2382-2390
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S4710 |
Picolinamide
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Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
- Neural Regen Res, 2023, 18(10):2252-2259
- Neural Regen Res, 2023, 18(10):2252-2259
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E1425 |
Nesuparib
|
Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. Nesuparib exhibits anti-tumor activity in BRCA-deficient xenograft models. |
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S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
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S6977 |
DR2313
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. |
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S6739 |
MN 64
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MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. |
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S0913 |
4',5,7-Trimethoxyflavone
|
4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein. |
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E1069 |
M2912
|
M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity. |
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S0732 |
GeA-69
|
GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. |
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S8993 |
Atamparib (RBN-2397)
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Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment. |
- bioRxiv, 2024, 2024.03.15.584457
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E1614New |
OUL232
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OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies. |
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S9893 |
Venadaparib(IDX-1197)
|
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. |
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E4869New |
Niraparib hydrochloride
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity. |
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S9360 |
4-Hydroxyquinazoline
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4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. |
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S8992 |
RBN012759
|
RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response. |
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S9875 |
Saruparib (AZD5305)
|
Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).
|
- Nature, 2024, 10.1038/s41586-024-07217-2
- Nature, 2024, 628(8007):433-441
- Nat Commun, 2024, 15(1):5822
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E2147 |
AZD9574
|
AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule. |
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S8876 |
RK-287107
|
RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. |
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