Transferase

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Transferase Inhibitors (9)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Clin Cancer Res, 2012, 18(13):3524-31
  • J Clin Endocrinol Metab, 2013, 98(6):2502-12
  • Stem Cells Transl Med, 2014, 3(4):510-9
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.
  • Biores Open Access, 2014, 3(4):176-82
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.
  • Mol Endocrinol, 2014, 28(3):395-405
  • Drug Des Devel Ther, 2015, 9:1555-84
  • Drug Des Devel Ther, 2015, 10.2147/DDDT.S75976
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.
  • Biosensors and Bioelectronics, 2014, 66:109-14
  • Lab Chip, 2014, 14(13):2354-62
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.
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.
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.
S7192 PF-04620110 PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1453 Tipifarnib <1 mg/mL 14 mg/mL <1 mg/mL
S2797 Lonafarnib <1 mg/mL 127 mg/mL 127 mg/mL
S2799 FK866 (APO866, Daporinad) <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
S7465 FTI 277 HCl 17 mg/mL 96 mg/mL 14 mg/mL
S4021 Tolcapone <1 mg/mL 55 mg/mL 55 mg/mL
S7467 LB42708 <1 mg/mL 100 mg/mL 86 mg/mL
S7192 PF-04620110 <1 mg/mL 49 mg/mL <1 mg/mL
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