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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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (170.6 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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