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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:
12352202
NACRES:
NA.77

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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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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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