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SML3252

Sigma-Aldrich

SF3B1 Protein Degrader

≥95% (HPLC)

Synonym(s):

2-((4-chlorophenyl)amino)-N-(6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)thiazole-4-carboxamide, O4I2-based PROTAC® degrader

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About This Item

Empirical Formula (Hill Notation):
C29H29ClN6O5S
Molecular Weight:
609.10
UNSPSC Code:
12352200

Quality Level

100

Assay

≥95% (HPLC)

form

powder

storage condition

under inert gas

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1N(C(C2=C1C=CC=C2NCCCCCCNC(C3=CSC(NC4=CC=C(C=C4)Cl)=N3)=O)=O)C5CCC(NC5=O)=O

Biochem/physiol Actions

SF3B1 Protein degrader (reported as "PROTAC-O4I2" in Gama-Brambila et al.) is a cell permeable degrader of splicing factor 3B1 (SF3B1) containing an SF3B1 activator O4I2 connected to the ligand of the cereblon ubiquitin ligase thalidomide. PROTAC-O4I2 selectively degrades SF3B1 in cells. It induces apoptosis of tumor cells and extends survival in Drosophila intestinal tumor model.

Legal Information

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Rodrigo A Gama-Brambila et al.
Cell chemical biology, 28(11), 1616-1627 (2021-05-29)
The proteolysis-targeting chimeras (PROTACs) are a new technology to degrade target proteins. However, their clinical application is limited currently by lack of chemical binders to target proteins. For instance, it is still unknown whether splicing factor 3B subunit 1 (SF3B1)

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