FTI-277 hydrochloride

• CAT Number: I002351
• CAS Number: 180977-34-8
• Molecular Formula: C₂₂H₂₉N₃O₃S₂.HCl
• Molecular Weight: 484.07
• Purity: ≥95%
• Target: Transferase
• Solubility: DMSO: ≥ 4.7 mg/mL
• Storage: 2-8°C
• IUPAC Name: methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylsulfanylbutanoate;hydrochloride
• InChI: InChI=1S/C22H29N3O3S2.ClH/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15;/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26);1H/t16-,20+;/m1./s1
• InChIKey: PIAFFJUUNXEDEW-PXPMWPIZSA-N
• SMILES: COC(=O)C(CCSC)NC(=O)C1=C(C=C(C=C1)NCC(CS)N)C2=CC=CC=C2.Cl

FTI 277 HCl（Cat No.:I002351）, the methyl ester of FTI 277, is a highly potent and selective inhibitor of farnesyltransferase (FTase), an enzyme involved in post-translational protein modification. With an impressive IC50 value of 500 pM, it exhibits remarkable inhibitory activity against FTase. Notably, FTI 277 HCl demonstrates a high level of selectivity, being 100-fold more specific for FTase than for the closely related enzyme geranylgeranyltransferase I (GGTase I). This selective inhibition of FTase makes FTI 277 HCl a promising candidate for targeted therapy and research in diseases related to aberrant protein farnesylation.

Reference

[1]. Cohen-Jonathan E, et al. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11.
[2]. Nakazawa H, et al. Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle. PLoS One. 2015 Jan 16;10(1):e0116633.
[3]. Virtanen SS, et al. Inhibition of GGTase-I and FTase disrupts cytoskeletal organization of human PC-3 prostate cancer cells. Cell Biol Int. 2010 Aug;34(8):815-26.