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CAM833

CAS No. : 2758364-02-0

產(chǎn)品活性：CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K_d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis.

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶點(diǎn)：RAD51  |  Apoptosis

In Vitro: CAM833 (3.125-50 μM; 24 h) causes a concentration-dependent decrease in RAD51 foci and subsequent increase in DNA damage.
CAM833 (25 μM) inhibits RAD51 molecular clustering at DNA damage sites and suppresses extended RAD51 filament assembly.
CAM833 (0-50 μM) inhibits DNA repair by homologous recombination.
CAM833 (20 μM; 0-72 h) potentiates radiation-induced cell-cycle arrest and increases apoptosis over time in HCT116 cells.
CAM833 (0.1-100 μM; 96 h) causes a dose-dependent growth inhibition of multiple cancer-derived human cell lines that is enhanced when combined with ionizing radiation.
CAM833 (20 μM; 96 h) potentiates the growth suppressive effect of PARP1 inhibition in BRCA2 wild-type cells.
CAM833 (96 h) alone inhibits the growth of HCT116 colon carcinoma cells with a GI₅₀ (50% growth inhibition) of 38 μM, when combined with 3 Gy IR, CAM833 suppresses the growth of HCT116 cells with a GI₅₀ of 14 μM.
The quinoline of CAM833 occupies a hotspot, the Phe-binding pocket on RAD51 and the methyl of the substituted α-methylbenzyl group occupies the Ala-binding pocket.

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