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Catalog No. Product Name Information Product Use Citations Product Validations
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
A5303 CHAT Rabbit Recombinant mAb CHAT Rabbit Recombinant mAb detects endogenous level of total CHAT.
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
Tags: Transferase activity | Transferase inhibition | Transferase activity | protein transferase | farnesyltransferase | DNA methyltransferase cancer | DNA methyltransferase activity | DNA methyltransferase assay | DNA methyltransferase mechanism | farnesyl transferase assay | Transferase inhibitor review