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SML3180

PZ15227

Name: PZ15227
Brand: SIGMA

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

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

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About This Item

Empirical Formula (Hill Notation):

C₇₁H₈₂ClF₃N₁₂O₁₂S₃

CAS Number:

2143464-25-7

Molecular Weight:

1484.13

UNSPSC Code:

12352200

NACRES:

NA.21

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

PZ15227, ≥98% (HPLC)

Quality Level

100

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

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

Related Categories

Bioactive Small Molecules

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number

0000176058

0000176059

0000176058

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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)

Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells.

Ryan Kolb et al.

Nature communications, 12(1), 1281-1281 (2021-02-26)

Regulatory T cells (Tregs) play an important role in maintaining immune homeostasis and, within tumors, their upregulation is common and promotes an immunosuppressive microenvironment. Therapeutic strategies that can eliminate Tregs in the tumor (i.e., therapies that do not run the

Osteocyte RANKL is required for cortical bone loss with age and is induced by senescence.

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

Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity.

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.

Global Trade Item Number

SKU	GTIN
SML3180-5MG	04065267214931
SML3180-25MG	04065267214924

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