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D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
2 mg | $44 | In Stock | |
5 mg | $70 | In Stock | |
10 mg | $128 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $411 | In Stock | |
100 mg | $597 | In Stock | |
1 mL x 10 mM (in DMSO) | $77 | In Stock |
Description | D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin. |
Targets&IC50 | RAD52:ki:25.8 µM |
In vitro | D-IO3 (0-10 μM; on Days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially inhibited the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner . D-IO3 inhibited cisplatin-induced RAD52 foci formation in the BCR-ABL1-positive BRCA1-deficient 32Dcl3 mouse hematopoietic cell line expressing GFP-RAD52. In the presence of D-IO3 (2.5 μM), the proportion of cells with RAD52 lesions decreased from 38.7% to 171%; meanwhile, the proportion of cisplatin-treated cells without lesions increased from 48.4% to 71.9%. D-IO3 had no effect on cisplatin-induced RAD51 foci. Similarly, D-I03 alone (in BRCA1-deficient cells) induced neither RAD51 nor RAD52 lesions, indicating that D-I03 has low genotoxicity[1]. |
In vivo | D-IO3 (50 mg / kg / day; intraperitoneal injection; daily; 7 consecutive days; nu / nu mice) treatment can reduce the growth of BRCA1-deficient MDA-MB-436 tumors. Talazoparib puls D-I03 does not cause any obvious toxicity to normal tissues and organs, and does not affect the growth of BRCA1-positive tumors. Pharmacokinetic and toxicity studies have shown that the maximum tolerated dose of D-I03 is ≥50mg / kg and t1 / 2 is 23.4 hours, resulting in a maximum concentration in peripheral blood> 1μM[1]. |
Alias | DI03 |
Molecular Weight | 428.64 |
Formula | C23H36N6S |
Cas No. | 688342-78-1 |
Smiles | CCN(CC)CCNC(=S)Nc1ccc2nc(cc(C)c2c1)N1CCN(CC)CC1 |
Relative Density. | 1.147 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90 mg/mL (210 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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