K-Ras(G12C) inhibitor 6
CAS No. | 2060530-16-5 | Cat. No. | BCP30805 |
Name | K-Ras(G12C) inhibitor 6 | ||
Synonyms | MDK30165; MDK-30165; MDK 30165; | ||
Formula | C17H22Cl2N2O3S | M. Wt | 405.34 |
Description | K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant. K-Ras (G12C) inhibitor 6 is a cysteine-reactive small molecule. It irreversibly binds to the G12C mutantion of GTPase K-Ras but not the wild-type K-Ras with the relative potency value of 4.2. The binding pocket of K-Ras for K-Ras (G12C) inhibitor 6 is a new allosteric pocket, S-IIP. Binding of this pocket results in a change of the relative nucleotide affinity of Ras to favour GDP over GTP, leading to an accumulation of inactive Ras. Since the mutation of K-Ras is quite common in human cancers, the inhibitor of K-Ras G12C should exert suppression activities in tumor cells. It has been reported that, some of the K-Ras G12C inhibitors are indeed effective to decrease cell viability and increase apoptosis in lung cancer cell lines. | ||
Pathways | GPCR/G Protein | ||
Targets | Ras/Rho |
Structure
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