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IOWH-032 (IOWH032) , a synthetic CFTR inhibitor, has been investigated for the treatment of cholera, diarrhea, and secretory diarrhea.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | $54 | In Stock | |
| 25 mg | $94 | In Stock | |
| 50 mg | $146 | In Stock | |
| 100 mg | $228 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $40 | In Stock |
| Description | IOWH-032 (IOWH032) , a synthetic CFTR inhibitor, has been investigated for the treatment of cholera, diarrhea, and secretory diarrhea. |
| Targets&IC50 | CFTR:1.01 μM |
| In vitro | In a closed-system mouse model, IOWH032 effectively inhibits the secretions induced by cholera toxin. Moreover, in a rat model with the cecum removed, IOWH032 (5 mg/kg) suppresses the excretion of waste. |
| In vivo | In T84-CFTR cells (IC50=6.87 μM), IOWH032 effectively inhibits CFTR activity. |
| Kinase Assay | Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1]. |
| Synonyms | IOWH032, IOWH 032 |
| Molecular Weight | 545.18 |
| Formula | C22H15Br2N3O4 |
| Cas No. | 1191252-49-9 |
| Smiles | Oc1c(Br)cc(cc1Br)-c1noc(n1)C(=O)NCc1ccc(Oc2ccccc2)cc1 |
| Relative Density. | 1.670 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (170.59 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.05 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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