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CFTR(inh)-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.
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Source | Oncotarget (2017). Figure 3. CFTRinh-172 |
| Method | Western-blot assay | |
| Cell Lines | K562 cells | |
| Concentrations | 20–50 μM | |
| Incubation Time | 24 h | |
| Results | Consistent with the results obtained using imatinib, CFTRinh-172 led to a significant reduction in p-BCR-ABL in both K562 and SUP-B15 cells as well as significant down-regulation oft-BCR-ABL in K562 cells (Figure 3A) but not in SUP-B15 cells (Figure 3C). |
| Molecular Weight | 409.4 |
| Formula | C18H10F3NO3S2 |
| CAS Number | 307510-92-5 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Zoia Kopeikin, et al. On the mechanism of CFTR inhibition by a thiazolidinone derivative
| Related CFTR Products |
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GLPG2737 is a potent CFTR type 2 corrector, and GLPG2737 can be used in combination with a type 1 co-corrector in the study of cystic fibrosis. |
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NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a agent used to treat cystic fibrosis that binds ΔF508-CFTR. |
| GLPG2737
GLPG2737 is a novel potent Type 2 corrector of CFTR. GLPG2737 showed high permeability both in MDCKII-MDRI and Caco-2 cells, with low efflux allowing an elevated absorbed fraction FaxFg and a dose proportional increase in exposure in rat from a dose of 5 to 300 mg/kg, despite a low aqueous thermodynamic solubility. |
| UCCF-853
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(R)-Posenacaftor sodium is the R-enantiomer of Posenacaftor and a cystic fibrosis transmembrane regulatory protein (CFTR) modulator that corrects the folding and transport of CFTR proteins.Posenacaftor is used in studies related to cystic fibrosis (CF). |
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