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Submit ReviewCAM 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.
分子量 | 528.97 |
公式 | C26H26ClFN4O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2758364-02-0 |
InChI Key | PMUWBFKMLGLUTF-KNUWZQJKSA-N |
Smiles | FC1=CC2=CC=C(N=C2C=C1)C(NCC(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=C(C=C(C=C4)OC)Cl)C)=O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 52.9 | 100 | |
ethanol | 2.64 | 5 |
以下数据基于产品分子量 528.97。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.89 mL | 9.45 mL | 18.9 mL |
5 mM | 0.38 mL | 1.89 mL | 3.78 mL |
10 mM | 0.19 mL | 0.95 mL | 1.89 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
Scott et al (2021) A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death. Cell Chem.Biol. 28 835 PMID: 33662256
If you know of a relevant reference for CAM 833, please let us know.
关键词: CAM 833, CAM 833 supplier, orthosteric, inhibitor, BRCA2, RAD51, interaction, DNA-damage, cancer, PARP1, selective, DNA,, RNA, and, Protein, Synthesis, 7457, Tocris Bioscience
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