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. |
|
|
S1453 |
Tipifarnib (R115777)
|
Tipifarnib (R115777, IND 58359) 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. |
-
Cancers (Basel), 2022, 14(4)903
-
Front Microbiol, 2021, 12:628283
-
Int Immunopharmacol, 2020, 3;83:106462
|
|
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. |
-
BMC Cancer, 2021, 21(1):252
-
Proc Natl Acad Sci U S A, 2019, 116(8):3126-3135
|
|
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 Neurosci, 2022, JN-RM-0449-21
-
Front Microbiol, 2021, 12:628283
-
Mol Cell, 2020, 80(1):164-174.e4
|
|
S2799 |
Daporinad (FK866, APO866)
|
Daporinad (FK866, APO866) 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 Res, 2022, 10.1038/s41422-022-00651-9
-
Dev Cell, 2022, 57(2):260-276.e9
-
Blood Cancer J, 2022, 12(3):39
|
|
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. |
|
|
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. |
-
Nat Commun, 2020, 11(1):5962
-
Sci Rep, 2020, 10(1):15556
-
Microbiol Immunol, 2020, 10.1111/1348-0421.12777
|
|
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. |
|
|
S4021 |
Tolcapone
|
Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
-
Viruses, 2021, 13(8)1533
|
|
S4189 |
Cyclandelate
|
Cyclandelate (BS 572) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
|
|
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.
|
|
|
S4589 |
Amodiaquine dihydrochloride dihydrate
|
Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent. |
-
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
-
J Med Chem, 2020, 31
-
bioRxiv, 2020, 10.1101/2020.04.13.039917
|
|
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. |
-
J Surg Res, 2021, 263:236-244
-
Exp Ther Med, 2015, 10(3):1066-1070
|
|
S4989 |
AOA hemihydrochloride
|
AOA hemihydrochloride (Aminooxyacetic acid, Carboxymethoxylamine, AOAA, Aminooxyacetate hemihydrochloride) is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor. |
-
Exp Cell Res, 2022, 411(1):113000
-
Biomed Rep, 2020, 13(2):3
-
Research Square, 2020, 10.21203/rs.3.rs-105979/v1
|
|
S5166 |
Benzoyleneurea
|
Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. Benzoyleneurea possesses anti-bacterial activity. |
|
|
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. |
|
|
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) |
|
|
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). |
|
|
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
|
|
S7465 |
FTI 277 HCl
|
FTI 277 HCl is the methyl ester of FTI 277, which 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. |
-
PLoS Biol, 2021, 19(4):e3001134
-
Cell Struct Funct, 2021, 46(1):1-9
-
Nat Commun, 2019, 10(1):273
|
|
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. |
-
Cell Struct Funct, 2021, 46(1):1-9
-
J Lipid Res, 2020, 61(12):1675-1686
-
Nat Commun, 2019, 10(1):273
|
|
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. |
|
|
S8244 |
Etomoxir sodium salt
|
Etomoxir sodium salt 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. |
-
Front Bioeng Biotechnol, 2022, 10:855755
-
J Cell Mol Med, 2022, 10.1111/jcmm.16879
-
Nat Commun, 2021, 12(1):5203
|
|
S8608 |
Adenosine Dialdehyde (ADOX)
|
Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM. |
-
PLoS Biol, 2022, 20(2):e3001535
-
Autophagy, 2021, 1-11
-
Autophagy, 2021, 1-11
|
|
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. |
-
STAR Protoc, 2022, 3(1):101113
|
|
S9231 |
Schisanhenol
|
Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
|
|
S9698 |
Ezatiostat
|
Ezatiostat (TER199, TLK199, Telintra), 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. |
|
|
S9835New |
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). |
-
Biomed Res Int, 2020, 2020:1921609
|
|
A5303 |
CHAT Rabbit Recombinant mAb
|
CHAT Rabbit Recombinant mAb detects endogenous level of total CHAT. |
|
|
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. |
|
|
S1453 |
Tipifarnib (R115777)
|
Tipifarnib (R115777, IND 58359) 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. |
- Cancers (Basel), 2022, 14(4)903
- Front Microbiol, 2021, 12:628283
- Int Immunopharmacol, 2020, 3;83:106462
|
|
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. |
- BMC Cancer, 2021, 21(1):252
- Proc Natl Acad Sci U S A, 2019, 116(8):3126-3135
|
|
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 Neurosci, 2022, JN-RM-0449-21
- Front Microbiol, 2021, 12:628283
- Mol Cell, 2020, 80(1):164-174.e4
|
|
S2799 |
Daporinad (FK866, APO866)
|
Daporinad (FK866, APO866) 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 Res, 2022, 10.1038/s41422-022-00651-9
- Dev Cell, 2022, 57(2):260-276.e9
- Blood Cancer J, 2022, 12(3):39
|
|
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. |
|
|
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. |
- Nat Commun, 2020, 11(1):5962
- Sci Rep, 2020, 10(1):15556
- Microbiol Immunol, 2020, 10.1111/1348-0421.12777
|
|
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. |
|
|
S4021 |
Tolcapone
|
Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
- Viruses, 2021, 13(8)1533
|
|
S4189 |
Cyclandelate
|
Cyclandelate (BS 572) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM. |
|
|
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.
|
|
|
S4589 |
Amodiaquine dihydrochloride dihydrate
|
Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent. |
- Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
- J Med Chem, 2020, 31
- bioRxiv, 2020, 10.1101/2020.04.13.039917
|
|
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. |
- J Surg Res, 2021, 263:236-244
- Exp Ther Med, 2015, 10(3):1066-1070
|
|
S4989 |
AOA hemihydrochloride
|
AOA hemihydrochloride (Aminooxyacetic acid, Carboxymethoxylamine, AOAA, Aminooxyacetate hemihydrochloride) is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor. |
- Exp Cell Res, 2022, 411(1):113000
- Biomed Rep, 2020, 13(2):3
- Research Square, 2020, 10.21203/rs.3.rs-105979/v1
|
|
S5166 |
Benzoyleneurea
|
Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. Benzoyleneurea possesses anti-bacterial activity. |
|
|
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. |
|
|
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) |
|
|
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). |
|
|
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
|
|
S7465 |
FTI 277 HCl
|
FTI 277 HCl is the methyl ester of FTI 277, which 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. |
- PLoS Biol, 2021, 19(4):e3001134
- Cell Struct Funct, 2021, 46(1):1-9
- Nat Commun, 2019, 10(1):273
|
|
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. |
- Cell Struct Funct, 2021, 46(1):1-9
- J Lipid Res, 2020, 61(12):1675-1686
- Nat Commun, 2019, 10(1):273
|
|
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. |
|
|
S8244 |
Etomoxir sodium salt
|
Etomoxir sodium salt 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. |
- Front Bioeng Biotechnol, 2022, 10:855755
- J Cell Mol Med, 2022, 10.1111/jcmm.16879
- Nat Commun, 2021, 12(1):5203
|
|
S8608 |
Adenosine Dialdehyde (ADOX)
|
Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM. |
- PLoS Biol, 2022, 20(2):e3001535
- Autophagy, 2021, 1-11
- Autophagy, 2021, 1-11
|
|
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. |
- STAR Protoc, 2022, 3(1):101113
|
|
S9231 |
Schisanhenol
|
Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
|
|
S9698 |
Ezatiostat
|
Ezatiostat (TER199, TLK199, Telintra), 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. |
|
|
S9835New |
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). |
- Biomed Res Int, 2020, 2020:1921609
|
|