PARP1 degrader-3
PARP1 degrader-3 is a selective PARP1 degrader derived from Olaparib (HY-10162) bearing a bicyclo[1.1.1]pentane (BCP) hydrophobic tag. PARP1 degrader-3 degrades PARP1 with a DC50 of 4.31 μM. PARP1 degrader-3 induces PARP1 degradation primarily through the ubiquitin-proteasome system, and the HSP70/HSP90-associated protein quality control pathway may be involved in this process. PARP1 degrader-3 can be used for colorectal cancer-related research.
For research use only. We do not sell to patients.
- Formula: C28H31FN4O3
- Molecular Weight:490.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PARP1 4.31 μM (DC50) |
PARP2 10 μM (DC50) |
In Vitro
PARP1 degrader-3 (compound 7i) (48 h) reduces SW620 cell viability with an IC50 of 5.62 μM[1].
PARP1 degrader-3 (1.25-20 μM; 24 h) decreases PARP1 protein levels in SW620 cells in a concentration-dependent manner, with a DC50 of 4.31 μM[1].
PARP1 degrader-3 (5 μM; 3-48 h) induces significant PARP1 degradation in SW620 cells starting at 6 h, with PARP1 protein reduced by more than 80% after 24 h and remaining at low levels up to 48 h[1].
PARP1 degrader-3 (5 μM; combined with MG132 (HY-13259), PS341 (HY-10227), or Chloroquine (HY-17589A)) induces PARP1 degradation in SW620 cells; MG132 and PS341 markedly attenuate this effect, whereas Chloroquine does not significantly affect PARP1 degradation, supporting its primary dependence on the ubiquitin-proteasome system[1].
PARP1 degrader-3 (5 μM; combined with HSP70 and/or HSP90 inhibitors) reduces PARP1 protein levels in SW620 cells; inhibition of HSP70 or HSP90 partially restores PARP1, and combined inhibition of both produces a more pronounced restoration effect[1].
PARP1 degrader-3 (0-3.2 μM; 24 h) decreases PARP1 protein levels in SW480 cells in a concentration-dependent manner[1].
PARP1 degrader-3 (0-10 μM; 24 h) decreases PARP1 protein levels in HT-29 cells in a concentration-dependent manner[1].
PARP1 degrader-3 (0-10 μM; 24 h) reduces PARP1 protein levels in HCT116 cells, with a more pronounced effect at 10 μM[1].
PARP1 degrader-3 (1.25-5 μM; 24 h) induces apoptosis in SW620 cells in a concentration-dependent manner, with the total apoptosis rate increasing from 9.64% in the control group to 22.04%, 42.3%, and 56.9%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620
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Concentration:0, 1.25, 2.5, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent degradation of PARP1 with a DC50 value of 4.31 μM.\nExhibited degradation selectivity toward PARP1 over PARP2 with a DC50 value of 10 μM for PARP2.
No significant degradation activity was observed against PARP3 and PARP5A.
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Cell Line:SW620
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Concentration:5 μM
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Incubation Time:0, 3, 6, 12, 24, 48 h
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Result:Produced evident PARP1 degradation from 6 h.
Depleted more than 80% of PARP1 protein after 24 h.
Maintained suppressed PARP1 levels through 48 h.
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Cell Line:SW620
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:24 h
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Result:Led to a concentration-dependent increase in apoptotic cell populations.
The overall apoptotic rate increased from 9.64% in the control group to 22.04%, 42.3%, and 56.9%.
The proportion of viable cells decreased from 88.3% to 42.3% at 5 μM.
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Cell Line:SW480
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Concentration:0, 0.2, 0.4, 0.8, 1.6, 3.2 μM
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Incubation Time:24 h
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Result:Markedly downregulated intracellular PARP1 protein levels.
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Cell Line:HT-29, HCT116
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Concentration:0, 5, 10 μM
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Incubation Time:24 h
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Result:Markedly downregulated intracellular PARP1 protein levels in HT-29 and HCT116 cells.
Chemical Information
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Molecular Weight 490.57
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Formula C28H31FN4O3
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SMILES
O=C(C1=C2C=CC=C1)NN=C2CC3=CC=C(F)C(C(NCCCCCCC(NC4C5CC4C5)=O)=O)=C3
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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)