2. Cell Cycle/DNA Damage Epigenetics PROTAC
  3. PARP PROTACs
  4. PROTAC PARP1 degrader-4

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)).

For research use only. We do not sell to patients.

PROTAC PARP1 degrader-4 Chemical Structure

PROTAC PARP1 degrader-4 Chemical Structure

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PROTAC PARP1 degrader-4 Related Antibodies

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Description

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787))[1].

IC50 & Target[1]

PARP1

 

In Vitro

PROTAC PARP1 degrader-4 (1-10 μM, 24-48 h) protects T47D and MOLT4 cells from gene toxicity-induced cell death[1].
PROTAC PARP1 degrader-4 (10 μM, 3-6 days) induces substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation[1].

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

PROTAC PARP1 degrader-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: Cardiomyocyte cell lines lacking BRCA1 mutations and MOLT4 cells
Concentration: 1, 5, 10 μM
Incubation Time: 144 h
Result: Showed minimal cytotoxicity in cardiomyocyte cell lines lacking BRCA1 mutations.
Induced substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation.
In Vivo

PROTAC PARP1 degrader-4 (40 mg/kg, i.p., 16 days) shows an anti-tumor effect in BRCA1-mutated MOLT4 xenografts mice[1].

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

Animal Model: 5-week-old NSG mice (injected 8 × 106 MOLT4 cells or 4 × 106 A2780)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), 16 days
Result: Exhibited a noticeable reduction in tumor size compared to the control group.
Effectively degraded PARP1 in tumors derived from MOLT4-xenografted mice.
Showed no significant alterations in neutrophil count, lymphocyte count or glutamic-pyruvic transaminase levels.
Molecular Weight

920.14

Formula

C51H62FN7O6S
SMILES

O=C1NCCC2=C(C3=CC=C(CN(C)C(CCCCCCCCC(N[C@H](C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)C(C)(C)C)=O)=O)C=C3)NC7=CC(F)=CC1=C72
Shipping

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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PROTAC PARP1 degrader-4 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:

PROTAC PARP1 degrader-4PARPPROTACspoly ADP ribose polymeraseMOLT4Anti-tumorT47DMDA-MB-231XenograftsOvarian and Breast cancer.Inhibitorinhibitorinhibit

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