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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. D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5 μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; while the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%.
| Molecular Weight | 428.64 |
| Formula | C23H36N6S |
| CAS Number | 688342-78-1 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA/RNA Synthesis Products |
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| Dencatistat
Dencatistat (P115) is an inhibitor of Cytidine Triphosphate Synthase 1 (CTPS1) with an IC50 value of ≤ 0.1 μM. |
| Antipain dihydrochloride
Antipain dihydrochloride is a protease inhibitor. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride also restricts uterine DNA synthesis and function in mice. |
| Tetrahydrouridine
Tetrahydrouridine (THU) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine. |
| Crisnatol
Crisnatol (BWA770U) is a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells. Crisnatol (BWA770U) is also an orally active and anticancer agent. |
| Caf1-IN-1
Caf1-IN-1 is inhibitor for ribonuclease Caf1 with an IC50 of 0.59 µM. Caf1-IN-1 is also a weak inhibitor for poly(A)-specific ribonuclease (PARN) with IC50 of 23.9 µM. |
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