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Submit ReviewBI 78D3 is a competitive c-Jun N-terminal kinase (JNK) inhibitor (IC50 = 280 nM) that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. Inhibits JNK interacting protein 1 (JIP1)-JNK binding (IC50 = 500 nM) and prevents JNK substrate phosphorylation. Blocks JNK-dependent Con A-induced liver damage and restores insulin sensitivity in a mouse model of type II diabetes.
BI 78D3 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 379.37 |
公式 | C13H9N5O5S2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 883065-90-5 |
PubChem ID | 2747117 |
InChI Key | QFRLDZGQEZCCJZ-UHFFFAOYSA-N |
Smiles | O=C1NN=C(SC3=NC=C([N+]([O-])=O)S3)N1C2=CC=C4C(OCCO4)=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.94 | 100 | |
ethanol | 1.9 | 5 |
以下数据基于产品分子量 379.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.64 mL | 13.18 mL | 26.36 mL |
5 mM | 0.53 mL | 2.64 mL | 5.27 mL |
10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Stebbins et al (2008) Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc.Natl.Acad.Sci.USA 105 16809 PMID: 1892277
Flight (2008) Getting rid of JNK. Nat.Rev.Drug Disc. 7 975
Haas and Writer (2008) Block JNK at the dock. SCiBX 1 1
If you know of a relevant reference for BI 78D3, please let us know.
关键词: BI 78D3, BI 78D3 supplier, Selective, competitive, JNK, inhibitors, inhibits, MAPK, Signaling, Signalling, c-Jun, N-Terminal, Kinases, SAPKs, Stress-Activated, Protein, Mitogen-Activated, p38, BI78D3, JNK/c-jun, 3314, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BI 78D3 的部分引用包括:
Eckle et al (2013) HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium. Br J Pharmacol 11 e1001665 PMID: 24086109
Gandham et al (2013) Effects of Y27632 on keratinocyte procurement and wound healing. Redox Biol 38 782 PMID: 23675999
Lahiri et al (2016) ERK2 phosphorylates Krüppel-like factor 8 protein at serine 48 to maintain its stability. Am J Cancer Res 6 910 PMID: 27293988
Jang et al (2015) Critical role of c-jun N-terminal protein kinase in promoting mitochondrial dysfunction and acute liver injury. PLoS Biol 6 552 PMID: 26491845
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.