iVeliparib-AP6 

iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC₅₀s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC₅₀s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism^[1][2]. (Pink: PARP-2 and PARP-1 ligand (HY-10129); Blue: Cereblon ligand (HY-41547); Black: linker (HY-120918)).

iVeliparib-AP6 (10 min) inhibits PARP1 and PARP2 catalytic activity in cell-free assays with IC₅₀ values of 69 nM and 21 nM, respectively^[1].

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

807.89

C₄₀H₅₃N₇O₁₁

2472645-27-3

O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCN3[C@](CCC3)(C4=NC5=CC=CC(C(N)=O)=C5N4)C)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Wang S, et al. Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation. Nat Chem Biol. 2019;15(12):1223-1231.  [Content Brief]

  [2]. Cao C, et al. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J Med Chem. 2020;63(19):11012-11033.  [Content Brief]