2472645-27-3
Chemical Structure
iVeliparib-AP6
- CAS No.: 2472645-27-3
- Formula:C40H53N7O11
- Molecular Weight:807.89
IUPAC Name: 2-((2R)-1-(20-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15,18-hexaoxaicosyl)-2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-7-carboxamide
InChIKey: XLGCZZCLPNSQNH-YMURELKOSA-N
SMILES: O=C1C2=C(NCCOCCOCCOCCOCCOCCOCCN3[C@](CCC3)(C4=NC5=CC=CC(C(N)=O)=C5N4)C)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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]
Keywords
