Chemical Structure : K-RAS4B inhibitor Cmpd2
CAS No.:
K-RAS4B inhibitor Cmpd2
Catalog No.: PC-24581Not For Human Use, Lab Use Only.
KRAS4B inhibitor Cmpd2 is a specific inhibitor of K-RAS4B, inhibtis the KRAS activation of BRAF with IC50 of 0.8 uM in coupled assays, and BLI Kd of <1 uM prenylated K-RAS4B in the presence of PS.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KRAS4B inhibitor Cmpd2 is a specific inhibitor of K-RAS4B, inhibtis the KRAS activation of BRAF with IC50 of 0.8 uM in coupled assays, and BLI Kd of <1 uM prenylated K-RAS4B in the presence of PS.
KRAS4B inhibitor Cmpd2 shows much affinity for the truncated, soluble GTPase domain of K-RAS determined by nuclear magnetic resonance (NMR) (Kd=700 uM).
Cmpd2 impairs the K-RAS4B interaction with the RBD of RAF on bilayers.
Cmpd2 inhibits BRAF activation by the prenylated form of the oncogenic K-RAS4B G12V mutant with EC50 of < 5 uM.
Physicochemical Properties
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M.Wt
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446.77
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Formula
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C21H21BrClN3O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-bromo-N-((2R,4S)-2-(4-chlorobenzyl)piperidin-4-yl)-1H-indole-3-carboxamide
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References
1. Fang Z, et al. Cell Chem Biol. 2018 Nov 15;25(11):1327-1336.e4.
2. Jansen JM, et al. PLoS One. 2017 Apr 6;12(4):e0174706.
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