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Merck
CN

SML3180

PZ15227

≥98% (HPLC), senolytic agent targeting BCL-XL protein, powder

别名:

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

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关于此项目

经验公式(希尔记法):
C71H82ClF3N12O12S3
化学文摘社编号:
分子量:
1484.13
UNSPSC Code:
12352200
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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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
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
Zhang P, et al.
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Nature communications, 12(1), 1281-1281 (2021-02-26)
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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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