Transferase

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.

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.

S2799

FK866 (APO866, Daporinad)

FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.

S2821

RG108

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

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.

S8244New

Etomoxir (Na salt)

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane.

S7466New

GGTI 298

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.

S4589New

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.

S4021

Tolcapone

Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.

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.

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.

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.

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.

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.

S2799

FK866 (APO866, Daporinad)

FK866 (APO866, Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.

S2821

RG108

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM in a cell-free assay, does not cause trapping of covalent enzymes.

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.

S8244New

Etomoxir (Na salt)

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane.

S7466New

GGTI 298

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.

S4589New

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.

S4021

Tolcapone

Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.

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.

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.

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.

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