Transferase

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1453 Tipifarnib <1 mg/mL 14 mg/mL <1 mg/mL
S2797 Lonafarnib <1 mg/mL 127 mg/mL 127 mg/mL
S2799 Daporinad (FK866, APO866) <1 mg/mL <1 mg/mL 78 mg/mL
S2821 RG108 <1 mg/mL 67 mg/mL 67 mg/mL
S2674 A922500 <1 mg/mL 86 mg/mL <1 mg/mL
S4743 Wogonin <1 mg/mL 56 mg/mL 8 mg/mL
S8244 Etomoxir (Na salt) 64 mg/mL 64 mg/mL 13 mg/mL
S7466 GGTI 298 <1 mg/mL 100 mg/mL 100 mg/mL
S4589 Amodiaquine dihydrochloride dihydrate 29 mg/mL 92 mg/mL <1 mg/mL
S4021 Tolcapone <1 mg/mL 55 mg/mL 55 mg/mL
S7467 LB42708 <1 mg/mL 100 mg/mL 86 mg/mL
S4280 Meclofenoxate (Centrophenoxine) HCl 58 mg/mL 58 mg/mL 58 mg/mL
S7192 PF-04620110 <1 mg/mL 49 mg/mL <1 mg/mL
S7465 FTI 277 HCl 17 mg/mL 96 mg/mL 14 mg/mL
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

Daporinad (FK866, APO866)

Daporinad (FK866, APO866) 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.

S4743New

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.

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

Daporinad (FK866, APO866)

Daporinad (FK866, APO866) 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.

S4743New

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.

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