S2799 |
Daporinad (FK866)
|
Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2. |
-
Cell Discov, 2024, 10(1):39
-
Theranostics, 2024, 14(7):2794-2815
-
Theranostics, 2024, 14(15):5999-6015
|
|
S8244 |
Etomoxir sodium salt
|
Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis. |
-
Bioact Mater, 2024, 35:549-563
-
Cell Chem Biol, 2024, 31(10):1772-1786.e5
-
Oncogene, 2024, 43(6):406-419
|
|
S1453 |
Tipifarnib
|
Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3. |
-
Cell Rep, 2023, 42(9):113098
-
iScience, 2023, 26(5):106695
-
Int J Mol Sci, 2023, 24(14)11546
|
|
S2797 |
Lonafarnib (SCH66336)
|
Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
-
J Cell Biol, 2024, 223(1)e202303007
-
J Cell Biol, 2024, 223(1)e202303007
-
EMBO Rep, 2024, 25(10):4311-4336
|
|
S7465 |
FTI 277 HCl
|
FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia. |
-
Cancer Res, 2023, 83(13):2248-2261
-
PLoS Biol, 2021, 19(4):e3001134
-
Cell Struct Funct, 2021, 46(1):1-9
|
|
S7466 |
GGTI 298 TFA salt
|
GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. |
-
bioRxiv, 2024, 10.1101/2024.01.16.575899
-
Nat Commun, 2023, 14(1):3251
-
Cell Struct Funct, 2021, 46(1):1-9
|
|
S4989 |
AOA (Aminooxyacetic acid) hemihydrochloride
|
AOA (Aminooxyacetic acid) hemihydrochloride is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor. |
-
Research Square, 2024, 10.21203/rs.3.rs-3849836/v1
-
Cell Rep Med, 2023, 4(5):101026
-
EMBO Mol Med, 2023, e15674.
|
|
S8608 |
ADOX (Adenosine Dialdehyde)
|
ADOX (Adenosine Dialdehyde) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM. |
-
Nat Commun, 2024, 15(1):8971
-
EMBO J, 2023, e114558.
-
PLoS Biol, 2022, 20(2):e3001535
|
|
S3021 |
Rimonabant (SR141716)
|
Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
-
Toxicol Lett, 2023, 374:48-56
-
Int J Biol Sci, 2022, 18(4):1401-1414
-
Mol Metab, 2022, 65:101597
|
|
S9870 |
STM2457
|
STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases. |
-
Nat Commun, 2024, 15(1):8539
-
Cell Rep, 2024, 43(2):113796
-
Cell Mol Biol Lett, 2024, 29(1):106
|
|
S7894 |
Tunicamycin
|
Tunicamycin, an antibiotic, can potently inhibit the N-linked glycosylation (NLG) by competitively inhibiting UDP-GlcNAc-dolichol-phosphate N-acetylglucosamine-1 phosphate transferase (DPAGT1) activity and can target several types of tumors by reducing angiogenesis, inhibiting colony formation, and enhancing TRAIL-induced apoptosis. |
-
Cell Discov, 2023, 9(1):92
-
Cell Discov, 2023, 9(1):92
-
Adv Sci (Weinh), 2023, 10(25):e2300414
|
|
S4589 |
Amodiaquine dihydrochloride dihydrate
|
Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent. |
-
Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
-
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
-
J Med Chem, 2020, 31
|
|
S8910 |
OSMI-4
|
OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells. |
-
Elife, 2023, 12e85595
-
Sci Adv, 2023, 9(33):eadg7112
-
Sci Adv, 2023, 9(33):eadg7112
|
|
S2674 |
A922500
|
A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
-
Nature, 2023, 621(7977):171-178
-
Nature, 2023, 621(7977):171-178
-
Cell Rep, 2022, 41(11):111827
|
|
S4021 |
Tolcapone
|
Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
-
FASEB J, 2022, 36(7):e22399
-
Viruses, 2021, 13(8)1533
-
Front Bioinform, 2021, 1:710591
|
|
S4743 |
Wogonin
|
Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase. |
-
Cancers -Basel, 2022, 14-174200
-
J Surg Res, 2021, 263:236-244
-
Exp Ther Med, 2015, 10(3):1066-1070
|
|
E0081 |
FIDAS-3
|
FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for methionine sadenosyltransferase 2A (MAT2A) binding . FIDAS-3 has anticancer activities by inhibiting the expression of oncogenes. FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for MAT2A.
|
-
Cell Death Dis, 2023, 14(8):525
-
Cell Death Dis, 2023, 14(8):525
|
|
S9954 |
SGN-2FF
|
SGN‐2FF (2-fluorofucose) is an orally bioavailable small‐molecule inhibitor of fucosyltransferase that demonstrated encouraging preclinical antitumor activity in mouse models. |
-
Aging Dis, 2023, 14(5):1927-1944
-
Aging Dis, 2023, 14(5):1927-1944
|
|
S7192 |
PF-04620110
|
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
-
J Pharm Biomed Anal, 2019, 170:176-186
-
J Cell Biol, 2018, 217(3):975-995
|
|
E0120 |
2-BP (2-Bromohexadecanoic acid)
|
2-BP (2-Bromohexadecanoic acid) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor, which inhibits multiple palmitoyl-acyl transferase (PAT) activity towards MyrGCK(NBD) and FarnCNRas(NBD) with identical IC50s of approx. 4 µM. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins. |
-
Cell Mol Biol Lett, 2024, 29(1):112
-
J Virol, 2024, 98(4):e0164923
-
Cancer Res, 2023, 83(12):2034-2051
|
|
S9835 |
OSMI-1
|
OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with IC50 of 2.7 μM for full length human OGT (ncOGT). |
-
Cell Death Dis, 2024, 15(4):244
-
Biomed Res Int, 2020, 2020:1921609
|
|
S2994 |
DL-Homocysteine
|
DL-Homocysteine is a weak neurotoxin that affects the production of kynurenic acid (KYNA) in the brain. DL-Homocysteine inhibits the activity of both KYNA biosynthetic enzymes, kynurenine aminotransferases (KATs) I and II. |
|
|
E1029 |
Miglustat
|
Miglustat (Zavesca, N‐butyldeoxynojirimycin, OGT 918) is an orally administered ceramide glucosyltransferase inhibitor which prevents the lysosomal accumulation of glucocerebroside. |
|
|
S9231 |
Schisanhenol
|
Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
-
Exploratory Research and Hypothesis in Medicine, 2023, 10.14218/ERHM.2023.00054
|
|
S0970 |
Curzerene
|
Curzerene, a sesquiterpene isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity, inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression and induces cell apoptosis. |
|
|
S9698 |
Ezatiostat
|
Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis. |
|
|
S5336 |
Hecogenin
|
Hecogenin (Hocogenin), a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM. |
|
|
S3945 |
L-Cycloserine
|
L-Cycloserine (Levcycloserine, Levcicloserina, Levcycloserinum, (-)-Cycloserine, (S)-Cycloserine) is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity. |
|
|
E0405 |
L002 (NSC764414)
|
L002 (NSC764414) is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. |
|
|
S5449 |
3-Methoxybenzamide
|
3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT) |
|
|
S0359 |
T863 (DGAT-3)
|
T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
|
|
E4639New |
FIDAS-5
|
FIDAS-5 is a potent and orally active inhibitor of methionine S-adenosyltransferase 2A (MAT2A) with an IC50 value of 2.1 μM, respectively. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 also demonstrates anticancer activity. |
|
|
S4189 |
Cyclandelate
|
Cyclandelate (BS 572,3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
|
|
S7467 |
LB42708
|
LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively. |
-
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
|
|
S5166 |
Benzoyleneurea
|
Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. |
|
|
S6886 |
1-Aminobenzotriazole
|
1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT). |
|
|
S4280 |
Meclofenoxate (Centrophenoxine) HCl
|
Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
|
|
|
S6392New |
SHIN1(RZ-2994)
|
SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels. |
|
|
S2799 |
Daporinad (FK866)
|
Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2. |
- Cell Discov, 2024, 10(1):39
- Theranostics, 2024, 14(7):2794-2815
- Theranostics, 2024, 14(15):5999-6015
|
|
S8244 |
Etomoxir sodium salt
|
Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis. |
- Bioact Mater, 2024, 35:549-563
- Cell Chem Biol, 2024, 31(10):1772-1786.e5
- Oncogene, 2024, 43(6):406-419
|
|
S1453 |
Tipifarnib
|
Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3. |
- Cell Rep, 2023, 42(9):113098
- iScience, 2023, 26(5):106695
- Int J Mol Sci, 2023, 24(14)11546
|
|
S2797 |
Lonafarnib (SCH66336)
|
Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
- J Cell Biol, 2024, 223(1)e202303007
- J Cell Biol, 2024, 223(1)e202303007
- EMBO Rep, 2024, 25(10):4311-4336
|
|
S7465 |
FTI 277 HCl
|
FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia. |
- Cancer Res, 2023, 83(13):2248-2261
- PLoS Biol, 2021, 19(4):e3001134
- Cell Struct Funct, 2021, 46(1):1-9
|
|
S7466 |
GGTI 298 TFA salt
|
GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. |
- bioRxiv, 2024, 10.1101/2024.01.16.575899
- Nat Commun, 2023, 14(1):3251
- Cell Struct Funct, 2021, 46(1):1-9
|
|
S4989 |
AOA (Aminooxyacetic acid) hemihydrochloride
|
AOA (Aminooxyacetic acid) hemihydrochloride is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor. |
- Research Square, 2024, 10.21203/rs.3.rs-3849836/v1
- Cell Rep Med, 2023, 4(5):101026
- EMBO Mol Med, 2023, e15674.
|
|
S8608 |
ADOX (Adenosine Dialdehyde)
|
ADOX (Adenosine Dialdehyde) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM. |
- Nat Commun, 2024, 15(1):8971
- EMBO J, 2023, e114558.
- PLoS Biol, 2022, 20(2):e3001535
|
|
S3021 |
Rimonabant (SR141716)
|
Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
- Toxicol Lett, 2023, 374:48-56
- Int J Biol Sci, 2022, 18(4):1401-1414
- Mol Metab, 2022, 65:101597
|
|
S9870 |
STM2457
|
STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases. |
- Nat Commun, 2024, 15(1):8539
- Cell Rep, 2024, 43(2):113796
- Cell Mol Biol Lett, 2024, 29(1):106
|
|
S7894 |
Tunicamycin
|
Tunicamycin, an antibiotic, can potently inhibit the N-linked glycosylation (NLG) by competitively inhibiting UDP-GlcNAc-dolichol-phosphate N-acetylglucosamine-1 phosphate transferase (DPAGT1) activity and can target several types of tumors by reducing angiogenesis, inhibiting colony formation, and enhancing TRAIL-induced apoptosis. |
- Cell Discov, 2023, 9(1):92
- Cell Discov, 2023, 9(1):92
- Adv Sci (Weinh), 2023, 10(25):e2300414
|
|
S4589 |
Amodiaquine dihydrochloride dihydrate
|
Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent. |
- Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
- Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
- J Med Chem, 2020, 31
|
|
S8910 |
OSMI-4
|
OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells. |
- Elife, 2023, 12e85595
- Sci Adv, 2023, 9(33):eadg7112
- Sci Adv, 2023, 9(33):eadg7112
|
|
S2674 |
A922500
|
A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
- Nature, 2023, 621(7977):171-178
- Nature, 2023, 621(7977):171-178
- Cell Rep, 2022, 41(11):111827
|
|
S4021 |
Tolcapone
|
Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
- FASEB J, 2022, 36(7):e22399
- Viruses, 2021, 13(8)1533
- Front Bioinform, 2021, 1:710591
|
|
S4743 |
Wogonin
|
Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase. |
- Cancers -Basel, 2022, 14-174200
- J Surg Res, 2021, 263:236-244
- Exp Ther Med, 2015, 10(3):1066-1070
|
|
E0081 |
FIDAS-3
|
FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for methionine sadenosyltransferase 2A (MAT2A) binding . FIDAS-3 has anticancer activities by inhibiting the expression of oncogenes. FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for MAT2A.
|
- Cell Death Dis, 2023, 14(8):525
- Cell Death Dis, 2023, 14(8):525
|
|
S9954 |
SGN-2FF
|
SGN‐2FF (2-fluorofucose) is an orally bioavailable small‐molecule inhibitor of fucosyltransferase that demonstrated encouraging preclinical antitumor activity in mouse models. |
- Aging Dis, 2023, 14(5):1927-1944
- Aging Dis, 2023, 14(5):1927-1944
|
|
S7192 |
PF-04620110
|
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
- J Pharm Biomed Anal, 2019, 170:176-186
- J Cell Biol, 2018, 217(3):975-995
|
|
E0120 |
2-BP (2-Bromohexadecanoic acid)
|
2-BP (2-Bromohexadecanoic acid) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor, which inhibits multiple palmitoyl-acyl transferase (PAT) activity towards MyrGCK(NBD) and FarnCNRas(NBD) with identical IC50s of approx. 4 µM. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins. |
- Cell Mol Biol Lett, 2024, 29(1):112
- J Virol, 2024, 98(4):e0164923
- Cancer Res, 2023, 83(12):2034-2051
|
|
S9835 |
OSMI-1
|
OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with IC50 of 2.7 μM for full length human OGT (ncOGT). |
- Cell Death Dis, 2024, 15(4):244
- Biomed Res Int, 2020, 2020:1921609
|
|
S2994 |
DL-Homocysteine
|
DL-Homocysteine is a weak neurotoxin that affects the production of kynurenic acid (KYNA) in the brain. DL-Homocysteine inhibits the activity of both KYNA biosynthetic enzymes, kynurenine aminotransferases (KATs) I and II. |
|
|
E1029 |
Miglustat
|
Miglustat (Zavesca, N‐butyldeoxynojirimycin, OGT 918) is an orally administered ceramide glucosyltransferase inhibitor which prevents the lysosomal accumulation of glucocerebroside. |
|
|
S9231 |
Schisanhenol
|
Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
- Exploratory Research and Hypothesis in Medicine, 2023, 10.14218/ERHM.2023.00054
|
|
S0970 |
Curzerene
|
Curzerene, a sesquiterpene isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity, inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression and induces cell apoptosis. |
|
|
S9698 |
Ezatiostat
|
Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis. |
|
|
S5336 |
Hecogenin
|
Hecogenin (Hocogenin), a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM. |
|
|
S3945 |
L-Cycloserine
|
L-Cycloserine (Levcycloserine, Levcicloserina, Levcycloserinum, (-)-Cycloserine, (S)-Cycloserine) is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity. |
|
|
E0405 |
L002 (NSC764414)
|
L002 (NSC764414) is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. |
|
|
S5449 |
3-Methoxybenzamide
|
3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT) |
|
|
S0359 |
T863 (DGAT-3)
|
T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
|
|
E4639New |
FIDAS-5
|
FIDAS-5 is a potent and orally active inhibitor of methionine S-adenosyltransferase 2A (MAT2A) with an IC50 value of 2.1 μM, respectively. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 also demonstrates anticancer activity. |
|
|
S4189 |
Cyclandelate
|
Cyclandelate (BS 572,3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
|
|
S7467 |
LB42708
|
LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively. |
- Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
|
|
S5166 |
Benzoyleneurea
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Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. |
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S6886 |
1-Aminobenzotriazole
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1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT). |
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S4280 |
Meclofenoxate (Centrophenoxine) HCl
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Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
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S6392New |
SHIN1(RZ-2994)
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SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels. |
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