2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. HyT PARP
  4. 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)).

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PARP1 degrader-2

PARP1 degrader-2 Chemical Structure

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PARP1 degrader-2 Related Antibodies

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Description

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))[1].

IC50 & Target[1]

PARP1

2.16 μM (DC50)

In Vitro

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.

PARP1 degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human triple-negative breast cancer MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10, 20 μM (concentration-dependent assay); 4 μM (time-dependent assay)
Incubation Time: 24 h (concentration-dependent assay); 3, 6, 12, 24, 48 h (time-dependent assay)
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.
Molecular Weight

627.75

Formula

C36H42FN5O4
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PARP1 degrader-2 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:

PARP1 degrader-2HyTPARPHydrophobie taggingpoly ADP ribose polymerasetriple-negative breast cancer cellsARG878PARP2ubiquitin-proteasome systemMDA-MB-468SW620PARP1BRCA1/2-proficient carcinoma-derived cell linesMDA-MB-231colon cancerInhibitorinhibitorinhibit

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PARP1 degrader-2
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