1622262-74-1
1622262-74-1 structure
- Name: BRCA1-IN-1
- Chemical Name: BRCA1-IN-1
- CAS Number: 1622262-74-1
- Molecular Formula: C27H33F2N4O6P
- Molecular Weight: 578.54
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2019-02-11 13:34:03
- Modify Date: 2024-01-10 11:16:21
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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.
| Name | BRCA1-IN-1 |
|---|
| Description | BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively. |
|---|---|
| Related Catalog | |
| 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]. |
| References |
| Molecular Formula | C27H33F2N4O6P |
|---|---|
| Molecular Weight | 578.54 |