Chemical Structure : CB-6644
CAS No.: 2316817-88-4
Catalog No.: PC-36002Not For Human Use, Lab Use Only.
CB-6644 (CB6644) is a potent, selective, allosteric, orally bioavailable inhibitor of the ATPase activity of RUVBL1/2 complex with IC50 of 15 nM.
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CB-6644 (CB6644) is a potent, selective, allosteric, orally bioavailable inhibitor of the ATPase activity of RUVBL1/2 complex with IC50 of 15 nM.
CB-6644 displays no appreciable activity against a panel of related AAA ATPases in ATPase assays (IC50>100 uM), including the p97.
CB-6644 binds to the RUVBL1/2 complex in an ATP-dependent manner.
CB-6644 interacts with the RUVBL1/2 complex in cells and induces cancer cell death in a panel of 123 cancer cell lines (EC50=41-785 nM), dose-dependently accumulates both p53 and p21 with EC50 of 0.24 and 0.15 uM in HCT116 cells.
CB-6644 demonstrates antitumor activity in xenograft tumor models.
M.Wt | 573.062 | |
Formula | C29H34ClFN4O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
5-chloro-2-ethoxy-4-fluoro-N-(4-((3-(methoxymethyl)-1-oxo-6,7-dihydro-1H,5H-benzo[c]pyrazolo[1,2-a][1,2]diazepin-2-yl)amino)-2,2-dimethyl-4-oxobutyl)benzamide |
1. Assimon VA, et al. ACS Chem Biol. 2019 Jan 14. doi: 10.1021/acschembio.8b00904.
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