Chemical Structure : KSQ-4279
CAS No.: 2446480-97-1
Catalog No.: PC-73318Not For Human Use, Lab Use Only.
KSQ-4279 (RO7623066) is a potent, selective, first-in-class inhibitor of USP1, shows anti-proliferative effects in a subset of cell lines, including mutations in BRCA1/2.
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KSQ-4279 (RO7623066) is a potent, selective, first-in-class inhibitor of USP1 with Ki of 1.2 nM, shows anti-proliferative effects in a subset of cell lines, including mutations in BRCA1/2.
KSQ-4279 has a unique mode of allosteric binding to USP1 and a high degree of selectivity over other family members.
USP1 is a protein regulating DNA damage response (DDR).
KSQ-4279 demonstrated efficacy both as a single agent and in combination with PARP inhibitors across multiple BRCA/HRD xenograft model.
M.Wt | 534.547 | |
Formula | C27H25F3N8O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
6-(4-Cyclopropyl-6-methoxypyrimidin-5-yl)-1-(4-(1-isopropyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-1H-pyrazolo[3,4-d]pyrimidine |
1. Sol Shenker, et al. Cancer Res (2021) 81 (13_Supplement): 1337.
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