1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

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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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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.

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7285 mL 8.6424 mL 17.2849 mL
5 mM 0.3457 mL 1.7285 mL 3.4570 mL
10 mM 0.1728 mL 0.8642 mL 1.7285 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

578.54

Formula

C₂₇H₃₃F₂N₄O₆P

CAS No.

1622262-74-1

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
BRCA1-IN-1
Cat. No.:
HY-100863
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BRCA1-IN-1

Cat. No.: HY-100863