688342-78-1
Chemical Structure
D-I03
- CAS. Nr.: 688342-78-1
- Formula:C23H36N6S
- Molecular Weight:428.64
IUPAC Name: 1-(2-(diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea
InChIKey: UXDGHRWOHOPKIL-UHFFFAOYSA-N
SMILES: S=C(NC1=CC=C2N=C(N3CCN(CC)CC3)C=C(C)C2=C1)NCCN(CC)CC
Biological Activity: D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 μM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 μM and 8 μM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin[1][2].
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D-I03 | 99.70% | D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 μM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 μM and 8 μM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin. | ||||||||||||||||||||
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- [1]. Huang F, et al. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Res. 2016 May 19;44(9):4189-99. [Content Brief]
- [2]. Hengel SR, et al. Small-Molecule Inhibitors Targeting DNA Repair and DNA Repair Deficiency in Research and Cancer Therapy. Cell Chem Biol. 2017 Sep 21;24(9):1101-1119. [Content Brief]
Keywords
