PARP1 degrader-2
PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)).
For research use only. We do not sell to patients.
- Formula: C36H42FN5O4
- Molecular Weight:627.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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PARP1 2.16 μM (DC50) |
PARP1 degrader-2 (Compound 11e) (serially diluted concentrations; 48 h) potently inhibits proliferation of MDA-MB-231 triple-negative breast cancer cells with an IC50 of 4.18 ± 0.30 μM[1].
PARP1 degrader-2 (Compound 11e) (serially diluted concentrations; 48 h) inhibits proliferation of SW620 colon cancer cells with an IC50 of 11.15 ± 0.18 μM[1].
PARP1 degrader-2 (Compound 11e) (serially diluted concentrations; 48 h) inhibits proliferation of MDA-MB-468 breast cancer cells with an IC50 of 6.96 ± 0.12 μM[1].
PARP1 degrader-2 (Compound 11e) (1.25-20 μM; 24 h) induces concentration- and time-dependent degradation of PARP1 in MDA-MB-231 cells, with a DC50 of 2.16 ± 0.29 μM at 24 h, and over 80% degradation achieved with 4 μM treatment for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human triple-negative breast cancer MDA-MB-231 cells
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Concentration:1.25, 2.5, 5, 10, 20 μM (concentration-dependent assay); 4 μM (time-dependent assay)
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Incubation Time:24 h (concentration-dependent assay); 3, 6, 12, 24, 48 h (time-dependent assay)
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Result:Induced concentration-dependent PARP1 degradation with a DC50 of 2.16 μM.
Detected PARP1 degradation after 6 h of treatment with 4 μM, with over 80% degradation observed at 24 h, and the degradative effect persisted for at least 48 h.
Chemical Information
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Molecular Weight 627.75
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Formula C36H42FN5O4
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SMILES
O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(CCCCCCC(NCC4CC5C=CC4C5)=O)=O)CC3)=O)=C2)C6=CC=CC=C61
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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 degrader-2 Related Classifications
HY-181460 Related Classifications
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