BI-78D3


Catalog No. size PriceQuantity
M6773-2 2mg solid $134
M6773-10 10mg solid $522

Description

Cas:883065-90-5

Product Information

BI-78D3, also known as JNK Inhibitor X, is a potent JNK inhibitor. BI-78D3 dose-dependently inhibits the phosphorylation of JNK substrates both in vitro and in cell. BI-78D3 not only blocks JNK dependent Con A-induced liver damage but also restores insulin sensitivity in mouse models of type 2 diabetes.

 

Synonyms

4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2,4-dihydro-5-((5-nitro-2-thiazolyl)thio)-3H-1,2,4-triazol-3-one

BI-78D3

 

Chemical Name:

 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2,4-dihydro-5-[(5-nitro-2-thiazolyl)thio]-3H-1,2,4-triazol-3-one

 

InChi Key: 

QFRLDZGQEZCCJZ-UHFFFAOYSA-N

 

InChi Code:

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)

 

Smiles Code:

O=C1NN=C(SC2=NC=C([N+]([O-])=O)S2)N1C3=CC=C(OCCO4)C4=C3

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

References

 

  1. Hein TW, Xu W, Xu X, Kuo L. Acute and Chronic Hyperglycemia Elicit JIP1/JNK-Mediated Endothelial Vasodilator Dysfunction of Retinal Arterioles. Invest Ophthalmol Vis Sci. 2016 Aug 1;57(10):4333-40. doi: 10.1167/iovs.16-19990. PubMed PMID: 27556216; PubMed Central PMCID: PMC5015966.

 

  1. Alaseem AM, Madiraju P, Aldebeyan SA, Noorwali H, Antoniou J, Mwale F. Naproxen induces type X collagen expression in human bone-marrow-derived mesenchymal stem cells through the upregulation of 5-lipoxygenase. Tissue Eng Part A. 2015 Jan;21(1-2):234-45. doi: 10.1089/ten.TEA.2014.0148. Epub 2014 Oct 23. PubMed PMID: 25091567; PubMed Central PMCID: PMC4292866.

 

  1. Posthumadeboer J, van Egmond PW, Helder MN, de Menezes RX, Cleton-Jansen AM, Beliën JA, Verheul HM, van Royen BJ, Kaspers GJ, van Beusechem VW. Targeting JNK-interacting-protein-1 (JIP1) sensitises osteosarcoma to doxorubicin. Oncotarget. 2012 Oct;3(10):1169-81. PubMed PMID: 23045411; PubMed Central PMCID: PMC3717953.

 

  1. Strittmatter F, Walther S, Gratzke C, Göttinger J, Beckmann C, Roosen A, Schlenker B, Hedlund P, Andersson KE, Stief CG, Hennenberg M. 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. doi: 10.1111/j.1476-5381.2012.01919.x. PubMed PMID: 22364229; PubMed Central PMCID: PMC3402815.

 

  1. Stebbins JL, De SK, Machleidt T, Becattini B, Vazquez J, Kuntzen C, Chen LH, Cellitti JF, Riel-Mehan M, Emdadi A, Solinas G, Karin M, Pellecchia M. 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. doi: 10.1073/pnas.0805677105. Epub 2008 Oct 15. PubMed PMID: 18922779; PubMed Central PMCID: PMC2567907.

 

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