YU238259 |
カタログ番号GC19390 |
Indirubin Derivative E804 は、インスリン様成長因子 1 受容体 (IGF1R) の強力な阻害剤であり、IGF1R の IC50 は 0.65 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1943733-16-1
Sample solution is provided at 25 µL, 10mM.
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD50 of 8.5 uM. YU238259 (0-5 uM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 uM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss[1].
YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice[1].
References:
[1]. Stachelek GC, et al. YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors. Mol Cancer Res. 2015 Oct;13(10):1389-97.
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