KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
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M.F/Formula | C108H182N44O25S2 |
M.W/Mr. | 2561.01 |
Activity | Inhibitor |
Biological Activity | KRpep-2d binds to K-Ras(G12D)with a Kd of 8.9 nM and approximately 6-fold selectivity over WT K-Ras, leading to an extended dissociation half-life. KRpep-2d significantly suppresses ERK-phosphorylation, downstream of K-Ras(G12D), along with A427 cancer cell proliferation at 30 μM peptide concentration. |
References | 1 Satoshi Sogabe, et al. ACS Med Chem Lett. 2017, 8:732−736. |
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