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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 |
|---|
| Ataluren
Ataluren (PTC124) is a novel, orally available small molecular CFTR-G542X nonsense allele inhibitor. |
| VX-770 (Ivacaftor)
VX-770 (Ivacaftor) is a first-in-class potentiator of CFTR, which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. |
| Lonidamine
Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). |
| VX-809
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell. |
| IOWH032
IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. |
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