iRucaparib-TP3
iRucaparib-TP3 is a non-trapping PARP1 PROTAC degrader with concurrent PARP1 catalytic inhibitory activity. iRucaparib-TP3 induces PARP1 ubiquitination and subsequent proteasomal degradation. iRucaparib-TP3 can be used for the research of cervical adenocarcinoma.
(Pink: PARP-1 ligand (HY-10617A); Blue: Cereblon ligand (HY-10984); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2410557-01-4
- Formel: C46H52FN9O8
- Molecular Weight:877.96
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PARP1 18 nM (IC50) |
In Vitro
iRucaparib-TP3 (0.1-20 μM; 24 h) induces highly specific degradation of PARP1 in HeLa cells with minimal off-target proteome perturbation[1].
iRucaparib-TP3 (1-5 μM; 24 h) abrogates PARP1 trapping on chromatin in HeLa cells by degrading PARP1, preventing detectable chromatin-bound PARP1 after methyl methanesulfonate-induced DNA damage[1].
iRucaparib-TP3 (48-72 h) does not induce DNA damage, G2 cell cycle arrest, or impaired cell proliferation in HeLa cells[1].
iRucaparib-TP3 (0.1-50 μM; 24 h) protects C2C12 myotubes, primary rat neonatal cardiomyocytes, and C2C12 myoblasts from genotoxic stress-induced NAD+ and ATP depletion without inducing PARP1 trapping, DNA damage, or impaired cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Induced PARP1 degradation in HeLa cells.
Chemical Information
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CAS. Nr. 2410557-01-4
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Molecular Weight 877.96
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Formel C46H52FN9O8
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SMILES
O=C1NCCC2=C(C3=CC=C(CN(C)CCCCC4=CN(CCOCCOCCOCCNC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)N=N4)C=C3)NC8=CC(F)=CC1=C82
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
iRucaparib-TP3 Related Classifications
HY-130645 Related Classifications
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