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FTase inhibitor I is a potent inhibitor of farnesyltransferase (FTase; IC₅₀ = 21 nM) that is greater than 30-fold selective for FTase over geranylgeranyl transferase (GGTase; IC₅₀ = 790 nM). It prevents farnesylation of Ras and inhibits proliferation of cells transformed by Ras farnesylation. In a dog model of subarachnoid hemorrhage, it reduces GTP-Ras in spastic basilar arteries, decreases angiographic vasospasm, and improves clinical scores.

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FTase Inhibitor I is a potent, selective, peptidomimetic FTase inhibitor.

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ChEBI: A dipeptide obtained from the tetrapeptide Cys-Val-Phe-Met by reduction of the amide carbonyl groups of the Cys and Val residues.

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This cell-permeable CAAX peptidomimetic (FW = 470.70 g/mol; FWtrifluoracetate-salt = 583.71 g/mol; CAS 149759-96-6), named as N-[2(S)- (2(R)-2-amino-3-mercaptopropylamino)-3-methylbutyl]-L-phenylalanyl-L methionine), binds to and prevents protein farnesyltransferase (IC50 = 21 nM) from interacting with C-terminal L-Cys-L-Val-L-Phe-L-Met substrate recognition sequences that are present in its natural substrates. Otherwise hydrophilic proteins associate with membranes by means of enzymatic attachment of hydrophobic moieties to their C-termini. Whereas prenylation occurs in the cytosol, post-prenylation processing is accomplished on the cytoplasmic surface of the endoplasmic reticulum and Golgi apparatus. B581 inhibits prenylation and processing of H-ras and lamin A. B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation.

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CONIER CHEM AND PHARMA LIMITED		sales@conier.com	China	49906	58
TargetMol Chemicals Inc.	+1-781-999-5354; +1-00000000000	marketing@targetmol.com	United States	32431	58
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BOC Sciences	16314854226; +8616314854226	inquiry@bocsci.com	United States	19852	58
Nextpeptide Inc	+86-0571-81612335 +8613336028439	sales@nextpeptide.com	China	19905	58
Nanjing TGpeptide	+86-13347807150	support@tgpeptide.com	China	3279	58
Aladdin Scientific		tp@aladdinsci.com	United States	52906	58
DAYANG CHEM (HANGZHOU) CO.,LTD	+86-88938639 +86-17705817739	info@dycnchem.com	China	53799	58
Shanghai Hanhong Scientific Co.,Ltd.	021-54306202 13764082696	info@hanhongsci.com	China	42917	64
Chemsky (shanghai) International Co.,Ltd	021-50135380	shchemsky@sina.com	China	15350	60

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