1. Cell Cycle/DNA Damage
  2. PARP
  3. BRCA1-IN-1


Cat. No.: HY-100863
Handling Instructions

BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.

For research use only. We do not sell to patients.

BRCA1-IN-1 Chemical Structure

BRCA1-IN-1 Chemical Structure

CAS No. : 1622262-74-1

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BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.

IC50 & Target

IC50: 0.53 μM (BRCA1)[1]
Ki: 0.71 μM (BRCA1)[1]

In Vitro

BRCTs are phosphoserine-binding domains found in proteins involved in DNA repair, DNA damage response and cell cycle regulation. BRCA1 is a BRCT domain-containing, tumor-suppressing protein expressed in the cells of breast and other tissues. By targeting the (BRCT)2 domain, BRCA1-IN-1 (Compound 15a) inhibits BRCA1 activities in tumor cells, sensitizes these cells to ionizing radiation-induced apoptosis, and shows synergistic inhibitory effect when used in combination with Olaparib (a small-molecule inhibitor of poly-ADP-ribose polymerase) and Etoposide (a small-molecule inhibitor of topoisomerase II). BRCA1-IN-1 can effectively inhibit HR activity by binding to BRCA1(BRCT)2, and functionally mimic genetic knockdown of BRCA1. BRCA1-IN-1 is useful in targeting BRCA1/PARP-related pathways involved in DNA damage and repair response, for cancer therapy. The synergistic inhibition of PARP/BRCA1 (a process referred to as synthetic lethality), is highly effective in cancer therapy. BRCA1-IN-1 is small-molecule-like and can be directly administered to tumor cells, thus making them useful for future studies of BRCA1/PARP-related pathways in DNA damage and repair response, and in cancer therapy[1].

Molecular Weight







O=C(N[[email protected]@H](CC(F)(F)P(O)(O)=O)C(NCC(NCCCCC1=CC=CC=C1)=O)=O)CCC2=CNC3=C2C=CC=C3


Room temperature in continental US; may vary elsewhere


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