D-I03

SKU: orb1709941

Description

D-I03 is a selective RAD52 inhibitor (Kd = 25.8 µM) that blocks RAD52-dependent SSA and D-loop formation (IC50 5 µM and 8 µM). It suppresses the growth of BRCA-deficient cells and inhibits damage-induced RAD52 foci formation in vitro, making it a research tool for studying homologous recombination repair pathways.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 688342-78-1
• MW: 428.64
• Purity: 99.04% (May vary between batches)
• Formula: C₂₃H₃₆N₆S
• SMILES: CCN(CC)CCNC(=S)Nc1ccc2nc(cc(C)c2c1)N1CCN(CC)CC1
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.7 mM);DMSO:90 mg/mL (209.97 mM)

Bioactivity

• Target IC50:
  D-loop:8 µM|RAD52:25.8 µM (Ki)|single-chain annealing (SSA):5 µM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RAD52, RNASynthesis, RNA Synthesis, DI 03, DI03, D-I03, DI-03, DNASynthesis, DNA Synthesis

Compound Identifiers

PubChem CID

24761372