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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.

Sinónimos:

CFTR Inhibitor III, OXO-172, 3-((3-Trifluoromethyl)phenyl)-5-((4-carboxyphenyl)methylene)-4-thiazolidinone, OXO-172

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About This Item

Fórmula empírica (notación de Hill):
C18H10F3NO4S
Peso molecular:
393.34
UNSPSC Code:
12352200

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

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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Nathaniel J Henning et al.
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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