ERK5-IN-1

Cat. No. 5393 1 次引用提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective ERK5 inhibitor

化学名： 11-Cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

纯度： ≥98% (HPLC)

引用文献 (1)

文献 (1)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for ERK5-IN-1

ERK5-IN-1 is a potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC₅₀ = 90 nM) and ERK5 enzymatic activity (IC₅₀ = 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable.

许可信息

Sold under license from Dana-Farber Cancer Institute.

化合物库 for ERK5-IN-1

ERK5-IN-1 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 ERK5-IN-1

分子量	638.8
公式	C₃₆H₄₆N₈O₃
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1435488-37-1
PubChem ID	71604307
InChI Key	XVBGRTMNFNMINE-UHFFFAOYSA-N
Smiles	O=C2N(C)C3=C(N=C(NC5=CC=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5OCC)N=C3)N(C4CCCC4)C1=CC=CC=C12

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 ERK5-IN-1

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	63.88	100
	ethanol	63.88	100

制备储备液 for ERK5-IN-1

以下数据基于产品分子量 638.8。 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	1.57 mL	7.83 mL	15.65 mL
5 mM	0.31 mL	1.57 mL	3.13 mL
10 mM	0.16 mL	0.78 mL	1.57 mL
50 mM	0.03 mL	0.16 mL	0.31 mL

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产品说明书 for ERK5-IN-1

分析证书/产品说明书

化学品安全技术说明书

参考文献 for ERK5-IN-1

参考文献是支持产品生物活性的出版物。

Deng et al (2013) Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur.J.Med.Chem. 70 758 PMID: 24239623

Elkins et al (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 56 4413 PMID: 23656407

If you know of a relevant reference for ERK5-IN-1, please let us know.

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关键词: ERK5-IN-1, ERK5-IN-1 supplier, potent, selective, ERK5, extracellular, regulated, kinases, MAPK7, inhibitors, inhibits, ERK, 5393, Tocris Bioscience

1 篇 ERK5-IN-1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 ERK5-IN-1 的部分引用包括：

C David et al (2019) Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas. Cancer Res 79 4026-4041 PMID: 31201162

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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 ERK5-IN-1

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.