PARP1/BRD4-IN-2
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC).
For research use only. We do not sell to patients.
- CAS No.: 3037993-97-5
- Formula: C25H20N4O4
- Molecular Weight:440.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD4 238 nM (IC50) |
PARP1 197 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
6.61 μM
Compound: BP44
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 35442700] |
| MDA-MB-468 | IC50 |
3.01 μM
Compound: BP44
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Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 35442700] |
PARP1/BRD4-IN-2 (compound BP44) can directly bind to BRD4 and PARP1 in MDA-MB-468 cells and improve their thermal stability[1].
PARP1/BRD4-IN-2 has antiproliferative activity against MDA-MB-231 and MDA-MB-468 with IC50s of 6.61±0.58 μM and 3.01±0.83 μM, respectively[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates Bcl-2 and up-regulates Bax and cleaved caspase3 at 20 μM; inhibits colony formation and promotes cell apoptosis in MDA-MB-468 cells[1].
PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates DNA damage-related proteins CtIP, Mre11, Rad51, and p-RPA32 dose-dependently; causes DNA damage repair defects by down-regulating Rad51 and p-RPA32[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Parameters of PARP1/BRD4-IN-2 in Sprague-Dawley rats[1].
| IV (1 mg/kg) | PO (10 mg/kg) | |
| T1/2 (h) | 3.02 ± 0.57 | 3.33 ± 0.71 |
| Cmax (ng/mL) | 258 ± 11 | 242 ± 6 |
| AUC0-t (ng/mL·h) | 629 ± 49 | 1489 ± 130 |
| AUC0-∞ (ng/mL·h) | 642 ± 36 | 1530 ± 146 |
| VZ (L/kg) | 21.1 ± 2.6 | |
| CL (mL/min/kg) | 33.7 ± 1.5 | |
| F (%) | 23.8 ± 1.3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (implanted subcutaneously with MDA-MB-468 tumor cells)[1]
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Dosage:40 and 80 mg/kg
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Administration:IG, for 16 days
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Result:Significantly inhibited tumor growth and exhibits no significant toxicities; and significantly down-regulated the expression of CtIP, c-Myc, PAR, and Rad51 in tumor tissues.
Chemical Information
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CAS No. 3037993-97-5
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Molecular Weight 440.45
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Formula C25H20N4O4
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SMILES
O=C1C2=CC=CC=C2C(CC3=CC=CC(C4=NC5=CC(OC)=CC(OC)=C5C(N4)=O)=C3)=NN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP1/BRD4-IN-2 Related Classifications
HY-150613 Related Classifications
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