Selective orthosteric inhibitor of the BRCA2-RAD51 interaction
CAM 833 a selective orthosteric inhibitor of the BRCA2-RAD51 interaction (Kd of 366 nM; IC50 of 6 μM). CAM 833 has no significant off-target interactions when screened at 10 μM in the Cerep ExpresSPanel. It inhibits DNA recombinase RAD51-mediated homologous recombination through binding to RAD51 at the same site as the BRCA2 FxxA motif. In cells, CAM 833 suppresses the assembly of RAD51 into damage-induced filaments at the sites of DNA damage. CAM 833 potentiates radiation-induced cytotoxicity and poly-ADP ribose polymerase (PARP)1 inhibitor- induced growth suppression in BRCA2-wild-type cells. The product is metabolically stable, does not significantly inhibit CYP450 enzymes, and is suitable for
in vivo
investigation.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124517 |
| Réf. fabricant | 18736156 |
| Nom chimique ou matériau | N-(2-((2 S,4 R)-2-((-1-(2-Chloro-4-methoxyphenyl)ethyl)carbamoyl)-4-hydroxypyrrolidin-1-yl)-2-oxoethyl)-6-fluoroquinoline-2-carboxamide |
| Quantité | 10 mg |
| Cible | DNA, RNA and Protein Synthesis Compounds |
| Formule moléculaire | C<sub>26</sub>H<sub>26</sub>ClFN<sub>4</sub>O<sub>5</sub> |
| Pureté | 0.98 |
