GGTI-286 hydrochloride

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GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC₅₀=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC₅₀s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC₅₀ of 1 μM.

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GGTI-286 hydrochloride Chemical Structure

CAS No. : 181141-66-2

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Other Forms of GGTI-286 hydrochloride:

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K-Ras H-Ras N-Ras Ras

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Description	GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC₅₀=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC₅₀s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC₅₀ of 1 μM^[1]^[2].
IC₅₀ & Target	IC50: 2 μM (Geranylgeranylation of Rap1A) in NIH3T3 cells^[1]
Molecular Weight	466.04
Formula	C₂₃H₃₂ClN₃O₃S
CAS No.	181141-66-2
SMILES	CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (268 KB) Handling Instructions (2659 KB)
References	[1]. E C Lerner, et al. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J Biol Chem. 1995 Nov 10;270(45):26770-3. [Content Brief] [2]. Naoyuki Nishiya, et al. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. Chem Biol. 2014 Apr 24;21(4):530-540. [Content Brief]