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About This Item
Empirical Formula (Hill Notation):
C13H9N5O5S2
CAS Number:
Molecular Weight:
379.37
MDL number:
UNSPSC Code:
12352200
Quality Level
Assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
−20°C
InChI
1S/C13H9N5O5S2/c19-11-15-16-12(25-13-14-6-10(24-13)18(20)21)17(11)7-1-2-8-9(5-7)23-4-3-22-8/h1-2,5-6H,3-4H2,(H,15,19)
InChI key
QFRLDZGQEZCCJZ-UHFFFAOYSA-N
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Stebbins, J.L., et al. 2008. Proc. Natl. Acad. Sci. USA105, 16809.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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