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PROTAC PARP1 degrader-3

PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for PARP1 with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC50 of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095) ; Pink: Ligand for target protein (HY-10619) ; Black: Linker (HY-16872) )

Product Specifications

UNSPSC

12352005

Target

PARP; PROTACs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-parp1-degrader-3.html

Smiles

NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CN(CCC5CCN(CCC6CCN(CC7CCN(C8=CC9=C(C(N(C%10CCC(NC%10=O)=O)C9=O)=O)C=C8)CC7)CC6)CC5)CCC4)C=C3)N=C21)=O

Molecular Formula

C52H65N9O5

Molecular Weight

896.13

References & Citations

[1]Wu M, et al., Discovery of a potent PARP1 PROTAC as a chemosensitizer for the treatment of colorectal cancer. Eur J Med Chem. 2025 Jan 15;282:117062.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PARP1

Frequently Asked Questions

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