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Submit ReviewXMD 8-92
说明： ERK5/BMK1 inhibitor; also BRD4 inhibitor
化学名： 2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
纯度： ≥98% (HPLC)
生物活性 for XMD 8-92
XMD 8-92 is an ERK5 (BMK1) and BRD4 inhibitor (Kd values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kd values are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. Also reduces BMK1-dependent transactivating activity of MEF2C. Inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.
许可信息
Sold under license from the Dana-Farber Cancer Institute.
External Portal Information for XMD 8-92
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of XMD 8-92 is reviewed on the chemical probes website.
化合物库 for XMD 8-92
XMD 8-92 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。
技术数据 for XMD 8-92
| 分子量 | 474.55 |
| 公式 | C26H30N6O3 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1234480-50-2 |
| PubChem ID | 46843772 |
| InChI Key | QAPAJIZPZGWAND-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OCC)C=C(N5CCC(O)CC5)C=C4)=NC=C1N2C |
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.
溶解性数据 for XMD 8-92
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 18.98 | 40 |
制备储备液 for XMD 8-92
以下数据基于产品分子量 474.55。 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 |
|---|---|---|---|
| 0.4 mM | 5.27 mL | 26.34 mL | 52.68 mL |
| 2 mM | 1.05 mL | 5.27 mL | 10.54 mL |
| 4 mM | 0.53 mL | 2.63 mL | 5.27 mL |
| 20 mM | 0.11 mL | 0.53 mL | 1.05 mL |
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产品说明书 for XMD 8-92
参考文献 for XMD 8-92
参考文献是支持产品生物活性的出版物。
Yang et al (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 18 258 PMID: 20832753
Yang and Lee (2011) Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin.Cancer Res. 17 3527 PMID: 21385929
Deng et al (2011) Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of big MAP kinase 1. ACS Med.Chem.Lett. 2 195 PMID: 21412406
Erazo et al (2013) Canonical and kinase activity-independent mechanisms for extracellular signal-regulated kinase 5 (ERK5) nuclear translocation require dissociation of Hsp90 from the ERK5-Cdc37 complex. Mol.Cell Biol. 33 1671 PMID: 23428871
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
If you know of a relevant reference for XMD 8-92, please let us know.
按产品操作查看相关产品
关键词: XMD 8-92, XMD 8-92 supplier, erk5, bmk1, big, MAP, kinase, 1, inhibitors, inhibits, antitumor, antiproliferative, antiproliferation, XMD8-92, bromodomains, BRD4, ERK, Bromodomains, 4132, Tocris Bioscience
8 篇 XMD 8-92 的引用文献
引用文献是使用了 Tocris 产品的出版物。 XMD 8-92 的部分引用包括：
Helmut et al (2021) ERK5 modulates IL-6 secretion and contributes to tumor-induced immune suppression. Cell Death Dis 12 969 PMID: 34671021
Simões et al (2015) Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation. Cell Death Dis 6 e1718 PMID: 25855966
C David et al (2019) Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas. Cancer Res 79 4026-4041 PMID: 31201162
Thompson et al (2018) Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma. Oncotarget 9 293 PMID: 29416614
Pereira et al (2016) MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism. Oncotarget 7 34322 PMID: 27144434
Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Mediators Inflamm 5 3145 PMID: 24762669
David S et al (2020) Slug regulates the Dll4-Notch-VEGFR2 axis to control endothelial cell activation and angiogenesis. Nat Commun 11 5400 PMID: 33106502
Jonathan A et al (2020) MEKK3-MEK5-ERK5 signaling promotes mitochondrial degradation. Cell Death Discov 6 107 PMID: 33101709
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该领域的文献
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。
MAPK Signaling Scientific Review
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.
Pathways for XMD 8-92
