化合物IOWH-032 T2486

Product Introduction
Bioactivity


英文名: IOWH-032

描述: IOWH-032 (IOWH032) 是一种合成 CFTR 抑制剂，可用于研究治疗霍乱、腹泻和分泌性腹泻，在T84和CHO-CFTR 细胞实验中IC50为1.01 uM。

激酶实验: 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].

体外活性: 在老鼠封闭系统模型中,IOWH032能够抑制霍乱毒素诱发的分泌物.切除盲肠的大鼠模型中, IOWH032（5 mg/kg）抑制排泄物排出.

体内活性: 在T84-CFTR细胞（IC50=6.87 μM）中,IOWH032能够抑制CFTR。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (170.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | SARS-CoV | IOWH-032 | Inhibitor | Cystic fibrosis transmembrane conductance regulator | SARS coronavirus | anti-diarrheal | CFBE41o- WT cells | CFTR | ACE-2

相关产品: GlyH-101 | Lumacaftor | (R)-BPO-27 | VRT-532 | Elexacaftor | Glibenclamide | Glucosamine | Ataluren | PG01 | Cavosonstat

相关库: Ion Channel Inhibitor Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途