2. Cell Cycle/DNA Damage
  3. RAD51
  4. BRCA2-RAD51-IN-3

BRCA2-RAD51-IN-3 is a RAD51-BRCA2 protein-protein interaction inhibitor with an EC50 of 29.35 μM and a Kd of 75.14 μM. BRCA2-RAD51-IN-3 blocks RAD51-BRCA2 binding, impairs homologous recombination in cancer cells, and induces synthetic lethality. BRCA2-RAD51-IN-3 acts in human pancreatic cancer cells and shows no activity in normal pancreatic cells. BRCA2-RAD51-IN-3 can be used for the research of pancreatic cancer.

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BRCA2-RAD51-IN-3

BRCA2-RAD51-IN-3 Chemical Structure

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BRCA2-RAD51-IN-3 Related Antibodies

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Description

BRCA2-RAD51-IN-3 is a RAD51-BRCA2 protein-protein interaction inhibitor with an EC50 of 29.35 μM and a Kd of 75.14 μM. BRCA2-RAD51-IN-3 blocks RAD51-BRCA2 binding, impairs homologous recombination in cancer cells, and induces synthetic lethality. BRCA2-RAD51-IN-3 acts in human pancreatic cancer cells and shows no activity in normal pancreatic cells. BRCA2-RAD51-IN-3 can be used for the research of pancreatic cancer[1].

In Vitro

BRCA2-RAD51-IN-3 (compound 19) inhibits the RAD51-BRCA2 protein-protein interaction in an in vitro ELISA assay with a EC50 of 29.35 μM and a maximum inhibition of 76%[1].
BRCA2-RAD51-IN-3 binds directly to recombinant human RAD51 with a Kd of 75.14 μM, as measured by MST[1].
BRCA2-RAD51-IN-3 (50 μM; 1 μM RAD51 plus 2-5 μM BRC4 peptide) binds to the RAD51-BRCA2 interaction interface, as confirmed by NMR displacement assays[1].
BRCA2-RAD51-IN-3 (10-80 μM) dose-dependently inhibits homologous recombination in BxPC-3 cells with an IC50 of 21.74 μM, reaching 81% inhibition at 80 μM[1].
BRCA2-RAD51-IN-3 (10-60 μM) inhibits homologous recombination in HEK-293 cells, reducing HR-proficient cells at 40 μM[1].
BRCA2-RAD51-IN-3 disrupts RAD51 foci formation in BxPC-3 cells after Cisplatin (HY-17394)-induced DNA damage, consistent with inhibition of RAD51-BRCA2-mediated DNA repair[1].
BRCA2-RAD51-IN-3 (40 μM; 6 days, in combination with 10 μM Olaparib (HY-10162) ) reduced cell viability synergistically in 2D BxPC-3 and HPAC cells (Interaction Index = 0.77 and 0.72, respectively), had no significant effect on the viability of normal H-6037 pancreatic epithelial cells, and induced apoptosis in BxPC-3 and HPAC cells as evidenced by a significantly increased BAX/BCL2 ratio.
BRCA2-RAD51-IN-3 (40-60 μM; 144 hours, in combination with 10 μM Olaparib) synergizes with Olaparib to reduce viability, inhibit growth, and induce cell death in BxPC-3 3D spheroids, with a 3D Interaction Index of 0.85 after 144 hours of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BRCA2-RAD51-IN-3 Related Antibodies

Cell Viability Assay[1]

Cell Line: BxPC-3 human pancreatic adenocarcinoma cells (2D culture)
Concentration: 40 μM (in combination with 10 μM olaparib)
Incubation Time: 6 days
Result: Had no significant effect on cell viability; in combination with olaparib, significantly enhanced antiproliferative activity with an Interaction Index of 0.77, indicating synergism.

Cell Viability Assay[1]

Cell Line: HPAC human pancreatic adenocarcinoma cells (2D culture)
Concentration: 40 μM (in combination with 10 μM olaparib)
Incubation Time: 6 days
Result: Had no significant effect on cell viability; in combination with olaparib, significantly enhanced antiproliferative activity with an Interaction Index of 0.72, indicating synergism.

Cell Viability Assay[1]

Cell Line: H-6037 normal human pancreatic epithelial cells (2D culture)
Concentration: 40 μM (in combination with 10 μM olaparib)
Incubation Time: 6 days
Result: The combination had no significant effect on cell viability.

Cell Viability Assay[1]

Cell Line: BxPC-3 human pancreatic adenocarcinoma cells (3D spheroid culture)
Concentration: 40-60 μM (in combination with 10 μM olaparib)
Incubation Time: 6 days
Result: Had no significant effect on spheroid viability or volume; in combination with olaparib, 60 μM significantly reduced spheroid viability and volume, and increased cell death, with a 3D Interaction Index of 0.85, indicating synergism.

Apoptosis Analysis[1]

Cell Line: BxPC-3 and HPAC human pancreatic adenocarcinoma cells
Concentration: 40 μM (in combination with 10 μM olaparib)
Incubation Time: 6 days
Result: Significantly increased the BAX/BCL2 ratio in both cell lines, indicating induction of apoptotic cell death.
Molecular Weight

367.33

Formula

C21H14NNaO4
SMILES

O=C(C1=CC(C2=CC=C(C3=CC=CC=C3)O2)=NC4=CC=C(OC)C=C14)O[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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References
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BRCA2-RAD51-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRCA2-RAD51-IN-3RAD51RAD51-BRCA2 protein-protein interactionhomologous recombinationhuman pancreatic cancer cellsnormal pancreatic cellsHEK-293 cellsHPAC cellsBxPC-3 cellssynthetic lethalitypancreatic cancerInhibitorinhibitorinhibit

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