1. Cell Cycle/DNA Damage
  2. PPAR
  3. iRucaparib-AP6

iRucaparib-AP6 

Cat. No.: HY-130644
Handling Instructions

iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.

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

iRucaparib-AP6 Chemical Structure

iRucaparib-AP6 Chemical Structure

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Description

iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1[1].

In Vitro

iRucaparib-AP6 (0-10 μM; 24 hours) decreases PARP-1 level in a dose dependent manner, exhibits a half-maximal degrading concentration (DC50) of 82 nM (Dmax = 92%)[1].
iRucaparib-AP6 (0-20 μM; 24 hours) induces degradation of PARP1 at low concentrations[1].

Cell Viability Assay[1]

Cell Line: Primary rat neonatal cardiomyocyte cells
Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased PARP-1 level in primary rat neonatal cardiomyocyte cells.

Western Blot Analysis[1]

Cell Line: Primary rat neonatal cardiomyocyte cells
Concentration: 0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM; 2 μM; 5 μM;10 μM; 20 μM
Incubation Time: 24 hours
Result: Induced robust PARP1 degradation at concentrations as low as 50 nM.
Molecular Weight

886.96

Formula

C₄₆H₅₅FN₆O₁₁

SMILES

O=C(NCC1)C2=CC(F)=CC3=C2C1=C(C4=CC=C(C=C4)CN(CCOCCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7CCC(NC7=O)=O)=O)=C5C6=O)C)N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

iRucaparib-AP6PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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iRucaparib-AP6
Cat. No.:
HY-130644
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