2143464-25-7
Chemical Structure
PZ15227
- CAS No.: 2143464-25-7
- Formula:C71H82ClF3N12O12S3
- Molecular Weight:1484.13
IUPAC Name: 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-(methylthio)-4-((2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yl)oxy)phenyl)urea
InChIKey: OWEARFNXBBNNKR-ADXOFTSBSA-N
SMILES: O=S(NC(C(C=C1)=CC=C1N2CCN(CC2)CC(CC(C)(CC3)C)=C3C4=CC=C(Cl)C=C4)=O)(C5=CC(S(=O)(C(F)(F)F)=O)=C(N[C@H](CCN6CCN(C(CCCN7N=NC(COCCOCCNC8=C9C(C(N(C9=O)C%10CCC(NC%10=O)=O)=O)=CC=C8)=C7)=O)CC6)CSC%11=CC=CC=C%11)C=C5)=O
Biological Activity: PZ15227 is a potent and selective Bcl-XL PROTAC degrader with a DC50 of 46 nM, and its Ki values for Bcl-XL, Bcl-2 and Bcl-w are 1.90 nM, 3.52 nM and >1 mM, respectively. PZ15227 recruits Bcl-XL to CRBN, induces polyubiquitination of Bcl-XL and promotes its proteasome-dependent degradation, thereby selectively killing senescent cells that rely on Bcl-XL for survival without causing severe thrombocytopenia. PZ15227 can be used for research related to age-related diseases, aging and renal cancer[1][2][3].
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PZ15227 | PZ15227 is a potent and selective Bcl-XL PROTAC degrader with a DC50 of 46 nM, and its Ki values for Bcl-XL, Bcl-2 and Bcl-w are 1.90 nM, 3.52 nM and >1 mM, respectively. PZ15227 recruits Bcl-XL to CRBN, induces polyubiquitination of Bcl-XL and promotes its proteasome-dependent degradation, thereby selectively killing senescent cells that rely on Bcl-XL for survival without causing severe thrombocytopenia. PZ15227 can be used for research related to age-related diseases, aging and renal cancer. | |||||||||||||||||||||
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References
- [1]. He Y, et al. Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity. Nature communications. 2020 Apr 24;11(1):1996.
- [2]. Kolb R, et al. Proteolysis-targeting chimera against BCL-X destroys tumor-infiltrating regulatory T cells. Nature communications. 2021 Feb 24;12(1):1281.
- [3]. Negi A, et al. Strategies to Reduce the On-Target Platelet Toxicity of Bcl-x Inhibitors: PROTACs, SNIPERs and Prodrug-Based Approaches. Chembiochem : a European journal of chemical biology. 2022 Jun 20;23(12):e202100689. [Content Brief]
