420140
JNK Inhibitor X, BI-78D3
4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
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Merck KGaA
Frankfurter Str. 250
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15 February 2012
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A cell-permeable benzodioxin-triazole compound that competes with JNK-interacting protein-1 (IC50 = 500 nM in competitive binding to JNK1 with pepJIP1) and D-domain-containing substrates binding (Ki = 200 nM in competitive binding to JNK1 with ATF2) by targeting JNK JIP1-interacting site (Kd = 8.1 µM). BI-78D3 inhibits the phosphorylation of ATF2, but not that of a D-domain-less peptide substrate, by JNK1 in kinase assays, while showing 100-fold less potency against p38α and no effect against mTOR or PI3-Kα. Shown to inhibit the TNF-α-stimulated GFP-cJun phosphorylation in transfected HeLa cultures in vitro (IC50 = 12.4 µM) and effectively reduce ConA-induced murine liver failure (10 mg/kg, i.p.) as well as restore insulin sensitivity in a murine type 2 diabetes model (25 mg/kg, i.p.) in vivo.
| Product information | |||
|---|---|---|---|
| Form | Pale yellow solid | ||
| Molar mass | 379.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C13H9N5O5S2 | ||
| CAS number | 883065-90-5 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Standard Handling |
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