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BI 78D3 Competitive JNK inhibitor

Catalog No.B9011
Size Price Stock Qty
5mg
$90.00
In stock
25mg
$350.00
In stock
50mg
$630.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BI 78D3

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Chemical Properties

Cas No. 883065-90-5 SDF Download SDF
Chemical Name 4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-((5-nitrothiazol-2-yl)thio)-4H-1,2,4-triazol-3-ol
Canonical SMILES OC1=NN=C(SC2=NC=C(S2)N(=O)=O)N1C3=CC4=C(OCCO4)C=C3
Formula C13H9N5O5S2 M.Wt 379.37
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

BI-78D3 is a substrate competitive inhibitor of JNK inhibitor [2].

JNK is a member of the MAPK family. JNK is a stress-activated protein kinase that modulates pathways implicated in a variety of disease states. Non-motoric JNK functions may differ between cell types and organs. The JNK is involved in a1-adrenoceptor-mediated contraction of prostate smooth muscle. For non-malignant, epithelial human prostate cells, JNK activation not only has the function of pro-apoptotic and antiproliferative but also related with JNK-dependent survival.[1]

BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In addition, it has been reported that BI-78D3 does not inhibit the phosphorylation of a short peptide substrate lacking a D-domain. This confirms that BI-78D3 is substrate competitive.[2]

BI-78D3 inhibits both noradrenaline- and phenylephrine-induced contractions. Then it prevents α1-adrenoceptor-mediated contraction of prostate tissue. As an effective JNK inhibitor, BI-78D3 has the ability of abrogating ConA-induced liver damage and restoring insulin sensitivity. [1,2]

References:
[1] Strittmatter F1, Walther S, Gratzke C, etal. , Inhibition of adrenergic human prostate smooth muscle contraction by the inhibitors of c-Jun N-terminal kinase, SP600125 and BI-78D3. Br J Pharmacol. 2012 Jul;166(6):1926-35.
[2] Stebbins JL, De SK, Machleidt T,etal.  , Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.