Transferase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Transferase Products

All (25) Transferase Inhibitors (25)

Catalog No.	Information	Product Use Citations	Product Validations
S1453	Tipifarnib Tipifarnib (R115777) 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.	Int Immunopharmacol, 2020, 3;83:106462 Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193	Effects of tipifarnib on GalN/LPS-induced mortality and ALF in mice. Representative liver histology (H/E staining at 5 h after saline or GalN/LPS) by microscopic images are shown.
S2797	Lonafarnib Lonafarnib 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.	Aging Cell, 2020, 29 Dev Biol, 2020, 457(2):215-225 Nat Cell Biol, 2018, 20(7):800-810	Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
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 Metab, 2020, 31(3):564-579 Mol Ther Nucleic Acids, 2020, 1;20:801-811 Front Cell Dev Biol, 2020, 17;8:191	Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.
S3021	Rimonabant Rimonabant 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.	Microbiol Immunol, 2020, 10.1111/1348-0421.12777
S2674	A922500 A922500 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.	Proc Natl Acad Sci U S A, 2019, 116(8):3126-3135
S0435^New	PF-9366 PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with IC50 of 420 nM and Kd of 170 nM.
S8056	Lomeguatrib Lomeguatrib is a potent inhibitor of O⁶-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.	Nucleic Acids Res, 2018, 46(20):10888-10904 Onco Targets Ther, 2018, 11:3671-3684 Mol Cancer Ther, 2015, 14(5):1236-46	Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B).
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.	Nat Commun, 2019, 10(1):273 Oncol Rep, 2018, 40(4):2171-2182
S8244	Etomoxir (Na 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.	Food Funct, 2020, 30;11(4):3361-3370 Nat Commun, 2019, 10(1):3856 Neoplasia, 2019, 21(7):713-720	Immunoblot analysis of CyclinD1, PCNA, γ-H2AX, cleaved-PRAP and -caspase3 (F) in normal saline or ETO-treated groups were determined at 10 weeks after HFD treatment (n = 10 mice/group).
S4021	Tolcapone Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with K_i of 30 nM.
S9231	Schisanhenol Schisanhenol is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7.
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.	J Med Chem, 2020, 31 bioRxiv, 2020, 2020/9/20.4.7.30734
S5336	Hecogenin Hecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM.
S4743	Wogonin Wogonin, 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.	Exp Ther Med, 2015, 10(3):1066-1070	Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; P<0.05 and **P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
S8608	Adenosine Dialdehyde (ADOX) Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
S3945	L-Cycloserine L-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity.
S5449	3-Methoxybenzamide 3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT)
S3658	O6-Benzylguanine O6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
S4189	Cyclandelate Cyclandelate 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.
S5166	Benzoyleneurea Benzoyleneurea scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. Benzoyleneurea possesses anti-bacterial activity.
S4989	AOA hemihydrochloride Aminooxyacetic acid is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism.	Biomed Rep, 2020, 13(2):3
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.
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.	Nat Commun, 2019, 10(1):273 Cancer Lett, 2018, 442:202-212 Oncol Rep, 2018, 40(4):2171-2182	(A) HCT 116 cells were treated with Tram (0, 30, or 60 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD. (B) SW480 and MDA-MB-231 cells were treated with Tram (0, 80, 160 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD.

Catalog No.	Information	Product Use Citations	Product Validations
S1453	Tipifarnib Tipifarnib (R115777) 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.	Int Immunopharmacol, 2020, 3;83:106462 Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193	Effects of tipifarnib on GalN/LPS-induced mortality and ALF in mice. Representative liver histology (H/E staining at 5 h after saline or GalN/LPS) by microscopic images are shown.
S2797	Lonafarnib Lonafarnib 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.	Aging Cell, 2020, 29 Dev Biol, 2020, 457(2):215-225 Nat Cell Biol, 2018, 20(7):800-810	Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
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 Metab, 2020, 31(3):564-579 Mol Ther Nucleic Acids, 2020, 1;20:801-811 Front Cell Dev Biol, 2020, 17;8:191	Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.
S3021	Rimonabant Rimonabant 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.	Microbiol Immunol, 2020, 10.1111/1348-0421.12777
S2674	A922500 A922500 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.	Proc Natl Acad Sci U S A, 2019, 116(8):3126-3135
S0435^New	PF-9366 PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with IC50 of 420 nM and Kd of 170 nM.
S8056	Lomeguatrib Lomeguatrib is a potent inhibitor of O⁶-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.	Nucleic Acids Res, 2018, 46(20):10888-10904 Onco Targets Ther, 2018, 11:3671-3684 Mol Cancer Ther, 2015, 14(5):1236-46	Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B).
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.	Nat Commun, 2019, 10(1):273 Oncol Rep, 2018, 40(4):2171-2182
S8244	Etomoxir (Na 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.	Food Funct, 2020, 30;11(4):3361-3370 Nat Commun, 2019, 10(1):3856 Neoplasia, 2019, 21(7):713-720	Immunoblot analysis of CyclinD1, PCNA, γ-H2AX, cleaved-PRAP and -caspase3 (F) in normal saline or ETO-treated groups were determined at 10 weeks after HFD treatment (n = 10 mice/group).
S4021	Tolcapone Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with K_i of 30 nM.
S9231	Schisanhenol Schisanhenol is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7.
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.	J Med Chem, 2020, 31 bioRxiv, 2020, 2020/9/20.4.7.30734
S5336	Hecogenin Hecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM.
S4743	Wogonin Wogonin, 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.	Exp Ther Med, 2015, 10(3):1066-1070	Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; P<0.05 and **P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
S8608	Adenosine Dialdehyde (ADOX) Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
S3945	L-Cycloserine L-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity.
S5449	3-Methoxybenzamide 3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT)
S3658	O6-Benzylguanine O6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
S4189	Cyclandelate Cyclandelate 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.
S5166	Benzoyleneurea Benzoyleneurea scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. Benzoyleneurea possesses anti-bacterial activity.
S4989	AOA hemihydrochloride Aminooxyacetic acid is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism.	Biomed Rep, 2020, 13(2):3
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.
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.	Nat Commun, 2019, 10(1):273 Cancer Lett, 2018, 442:202-212 Oncol Rep, 2018, 40(4):2171-2182	(A) HCT 116 cells were treated with Tram (0, 30, or 60 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD. (B) SW480 and MDA-MB-231 cells were treated with Tram (0, 80, 160 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD.

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Inhibitory Selectivity

Transferase Products