219672
CFTR Inhibitor III, OXO-172
The CFTR Inhibitor III, OXO-172 controls the biological activity of CFTR. This small molecule/inhibitor is primarily used for Biochemicals applications.
Synonym(s):
CFTR Inhibitor III, OXO-172, 3-((3-Trifluoromethyl)phenyl)-5-((4-carboxyphenyl)methylene)-4-thiazolidinone, OXO-172
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About This Item
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Quality Level
Assay
≥95% (HPLC, NMR)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
ethanol: 1 mg/mL
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable CFTRinh-172 (Cat. No. 219670) 2-oxo analog that exhibits ~25-fold higher aqueous solubility than the 2-thioxo CFTRinh-172 (420 µM vs. 17 µM, respectively, in PBS with 2% DMSO at 25 °C) and great potency, albeit slightly weaker than that of CFTRinh-172, in inhibiting CFTR-mediated apical membrane chloride current upon 20 µM Forskolin (Cat. No. 344270) stimulation in CFTR-expressing FRT cells (IC50 = 1.4 µM vs. 0.38 µM with CFTRinh-172) with practically no cytotoxicity (91% of no-drug control FRT in viability assay; 48 h at 50 µM).
A cell-permeable CFTRinh-172 (Cat. No. 219670) 2-oxo analog that exhibits ~25-fold higher aqueous solubility than the 2-thioxo CFTRinh-172 (420 µM vs. 17 µM, respectively, in PBS with 2% DMSO at 25 °C) and great potency, albeit slightly weaker than that of CFTRinh-172, in inhibiting CFTR-mediated apical membrane chloride current upon 20 µM Forskolin (Cat. No. 344270) stimulation in CFTR-expressing FRT cells (IC50 = 1.4 µM vs. 0.38 µM with CFTRinh-172) with practically no cytotoxicity (91% of no-drug control FRT in viability assay; 48 h at 50 µM).
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Sonawane, N.D., and Verkman, A.S. 2008. Bioorg. Med. Chem.16, 8187.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Nature chemical biology, 18(4), 412-421 (2022-02-26)
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we present deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a
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