产品名称
PZ15227, ≥98% (HPLC)
InChI
1S/C71H82ClF3N12O12S3/c1-70(2)27-25-57(48-13-17-51(72)18-14-48)50(43-70)44-83-33-35-84(36-34-83)54-19-15-49(16-20-54)66(90)80-102(96,97)56-21-22-59(62(42-56)101(94,95)71(73,74)75)77-52(47-100-55-8-4-3-5-9-55)26-30-82-31-37-85(38-32-82)64(89)12-7-29-86-45-
InChI key
OWEARFNXBBNNKR-ADXOFTSBSA-N
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Bcl-xl specific PROTAC that potently targets Bcl-xl for degradation by cereblon E3 ligase
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
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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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