All Photos(1)
Synonym(s):
4-[4-[[2-(4-Chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-[4-[4-[4-[[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]methyl]-1H-1,2,3-triazol-1-yl]-1-oxobutyl]-1-piperazinyl]-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]phenyl]sulfonyl]benzamide, PZ 15227
Empirical Formula (Hill Notation):
C71H82ClF3N12O12S3
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC1(C)CCC(C2=CC=C(Cl)C=C2)=C(CN3CCN(C4=CC=C(C(NS(C5=CC=C(N[C@@H](CSC6=CC=CC=C6)CCN7CCN(C(CCCN8C=C(COCCOCCNC9=C%10C(C(N(C%11CCC(NC%11=O)=O)C%10=O)=O)=CC=C9)N=N8)=O)CC7)C(S(C(F)(F)F)(=O)=O)=C5)(=O)=O)=O)C=C4)CC3)C1
General description
PZ15227 is a proteolysis targeting chimeras (PROTACs) based senolytic agent targeting BCL-XL protein. It is a derivative of ABT-263, a Bcl-2 family protein inhibitor. PZ15227 degrades Bcl-xl by recruiting celebron (CRBN) E3 ligase in senescent cells but not in platelets. Comparative to its parent compound, PZ15227 is less toxic to human platelets because of low CRBN expression in platelets.
Biochem/physiol Actions
Bcl-xl specific PROTAC that potently targets Bcl-xl for degradation by cereblon E3 ligase
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Certificates of Analysis (COA)
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PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
Zhang P, et al.
Exploration of targeted anti-tumor therapy, 1(4), 259-272 (2020)
Ha-Neui Kim et al.
JCI insight, 5(19) (2020-09-02)
In aging mice, osteoclast number increases in cortical bone but declines in trabecular bone, suggesting that different mechanisms underlie age-associated bone loss in these 2 compartments. Osteocytes produce the osteoclastogenic cytokine RANKL, encoded by Tnfsf11. Tnfsf11 mRNA increases in cortical
Yonghan He et al.
Nature communications, 11(1), 1996-1996 (2020-04-26)
Small molecules that selectively kill senescent cells (SCs), termed senolytics, have the potential to prevent and treat various age-related diseases and extend healthspan. The use of Bcl-xl inhibitors as senolytics is largely limited by their on-target and dose-limiting platelet toxicity.
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