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Submit ReviewAX 15836 is a potent and selective ERK5 inhibitor (IC50 = 8 nM). Exhibits >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Also exhibits selectivity over bromodomain BRD4 (Kd = 3,600 nM). Increases vomocytosis in human macrophages in vitro, as well as in an in vivo zebrafish model of cryptococcal disease, reducing spread of infection.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of AX15836 is reviewed on the chemical probes website.
AX 15836 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 648.78 |
公式 | C32H40N8O5S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2035509-96-5 |
PubChem ID | 122705989 |
InChI Key | HTFNVAVTYILUCF-UHFFFAOYSA-N |
Smiles | CCOC1=C(NC2=NC=C3N(C)C(=O)C4=C(C=CC=C4)N(C3=N2)S(C)(=O)=O)C=CC(=C1)C(=O)N1CCC(CC1)N1CCN(C)CC1 |
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 | |||
1eq. HCl | 64.88 | 100 | |
DMSO | 64.88 | 100 |
以下数据基于产品分子量 648.78。 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 | 1.54 mL | 7.71 mL | 15.41 mL |
5 mM | 0.31 mL | 1.54 mL | 3.08 mL |
10 mM | 0.15 mL | 0.77 mL | 1.54 mL |
50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
参考文献是支持产品生物活性的出版物。
Lin et al (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 113 11865 PMID: 27679845
Gilbert et al (2017) Vomocytosis of live pathogens from macrophages is regulated by the atypcial MAP kinase ERK5. Sci.Adv. 3 e1700898 PMID: 28835924
If you know of a relevant reference for AX 15836, please let us know.
关键词: AX 15836, AX 15836 supplier, AX15836, potent, selective, ERK5, inhibitors, inhibits, vomocytosis, ERK, 5843, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AX 15836 的部分引用包括:
Ignacio et al (2020) CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci. Cell Rep 33 108545 PMID: 33357429
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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.