RAD51 Inhibitor B02

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种特异性人RAD51重组酶抑制剂，IC50为27.4 uM；对大肠杆菌同源物 RecA 无活性 (IC50>250 uM)。

A specific human RAD51 recombinase inhibitor with IC50 of 27.4 uM; shows no activity against E. coli homologue RecA (IC50>250 uM), disrupts RAD51 binding to DNA and specifically inhibits the DNA strand exchange activity of human RAD51; inhibits homologous recombination (HR) and increases cell sensitivity to DNA damage, sensitizes multiple myeloma cells to doxorubicin.

RAD51 Inhibitor B02 specifically inhibits human RAD51 (IC50=27.4 μM), but not its E. coli homologue RecA (IC50>250 μM). The combination of B02 with cisplatin has the strongest killing effect on the human breast cancer cells MDA-MB-231.

B02 significantly enhances the therapeutic effect of cisplatin on tumor cells in vivo. B02 is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No inhibition of tumor growth is observed on mice solely treated by B02. Mice treated with 4 mg/kg cisplatin, however, shows a 33% inhibition of tumor growth. Finally, mice treated with 50 mg/kg B02 and 4 mg/kg cisplatin shows a 66% inhibition of tumor growth.

B02 | B-02 | B 02

Cell Cycle/DNA Damage

RAD51

RAD51

——

——

1290541-46-6

339.38988

C22H17N3O

>98% (HPLC)

DMSO: ≥ 37 mg/mL

O=C1N(CC2=CC=CC=C2)C(/C=C/C3=CC=CN=C3)=NC4=C1C=CC=C4

4(3H)-Quinazolinone, 3-(phenylmethyl)-2-[(1E)-2-(3-pyridinyl)ethenyl]-

(-20℃)

With Ice Pack

≥ 2 years