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662005 Sigma-AldrichU0126 - CAS 109511-58-2 - Calbiochem

U0126, CAS 109511-58-2, is a potent and specific inhibitor of MEK1 (IC₅₀ = 72 nM) and MEK2 (IC₅₀ = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK.

U0126 - CAS 109511-58-2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
小册子
数据表
Data Sheet
Citations

同义词: 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI

Primary Target: MEK1 and MEK2

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
109511-58-2	C₁₈H₁₆N₆S₂•½C₂H₅OH

价格及供货情况

产品目录编号	库存情况	包装	数量 / 包装	价格	数量
662005-10MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	塑胶安瓿;塑胶针药瓶	10 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹
662005-1MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	玻璃瓶	1 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹
662005-20MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	塑胶安瓿;塑胶针药瓶	20 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹
662005-5MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	玻璃瓶	5 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹

Description
Overview	A potent and specific inhibitor of MEK1 (IC₅₀ = 72 nM) and MEK2 (IC₅₀ = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK. Has very little effect on other kinases such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. Also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution™ format (Cat. No. 662009).
Catalogue Number	662005
Brand Family	Calbiochem®
Synonyms	1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI

References
References	Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232. DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175. Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839. Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

Product Information
CAS number	109511-58-2
ATP Competitive	N
Form	White solid
Hill Formula	C₁₈H₁₆N₆S₂•½C₂H₅OH
Chemical formula	C₁₈H₁₆N₆S₂•½C₂H₅OH
Reversible	N
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	MEK1 and MEK2
Primary Target IC<sub>50</sub>	72 nM, 58 nm, against MEK1, and MEK2, respectively
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	N

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Unstable in solution; reconstitute just prior to use.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
662005-10MGCN	04055977261691
662005-1MGCN	07790788052249
662005-20MGCN	04055977261004
662005-5MGCN	04055977261011

Documentation

U0126 - CAS 109511-58-2 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

U0126 - CAS 109511-58-2 - Calbiochem 分析证书

标题	批号
662005	输入批号

参考

参考信息概述
Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232. DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175. Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839. Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

小册子

标题
An Introduction to Inhibitors and Their Biological Applications - 1st Edition

数据表

标题
Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation

引用

标题

Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232.

Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953.

Chengyu Wu and Jiaoti Huang. 2007. Journal of Biological Chemistry 282, 3571.

Alexandra Thiel, Mira Heinonen, Johanna Rintahaka, Tuija Hallikainen, and Annabrita Hemmes, Dan A. Dixon, Caj Haglund, and Ari Ristimaki. (2006) EXPRESSION OF CYCLOOXYGENASE-2 IS REGULATED BY GSK-3 IN GASTRIC CANCER CELLS. Journal of Biological Chemistry in press,.

Thiel, A., et al. 2006. Journal of Biological Chemistry 281, 4564.

Basak, C., et al. 2005. Journal of Immunology 174, 5672.

Soonkyu Chung, et al. (2005) Conjugated linoleic acid promotes human adipocyte insulin resistance through NF-κB-dependent cytokine production. Journal of Biological Chemistry 280, 38445-38456.

Marie-Claire Delfini, et al. (2005) Control of the segmentation process by graded MAPK/ERK activation in the chick embryo. Proceedings of the National Academy of Science USA 102, 11343-11348.

Gutzmer, R., et al. 2005. Journal of Immunology 5224.

Monick, M.M., et al. 2005. Journal of Biological Chemistry 280, 2147.

Tang, Q-Q., et al. 2005. Proceedings of the National Academy of Sciences (USA) 102, 9766.

Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432.

Wojciechowski, W., et al. 2005. Journal of Immunology 174, 7859.

Wu, M-H., et al. 2005. The Journal of Clinical Endocrinology & Metabolism 90, 286.

Yung-Luen Yu, et al. (2005) MAP kinase-mediated phosphorylation of GATA-1 promotes Bcl-XL expression and cell survival. Journal of Biological Chemistry 280, 29533-29542.

Naoto Inukai, et al. (2004) A novel hydrogen peroxide-induced phosphorylation and ubiquitination pathway leading to RNA polymerase II proteolysis. Journal of Biological Chemistry 279, 8190-8195.

Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385.

Michael J. Cross, et al. (2002) The Shb Adaptor Protein Binds to Tyrosine 766 in the FGFR-1 and Regulates the Ras/MEK/MAPK Pathway via FRS2 Phosphorylation in Endothelial Cells. Molecular Biology of the Cell 13, 2881-2893.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	28-February-2012 RFH
Synonyms	1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI
Description	A potent and specific inhibitor of MEK1 (IC₅₀ = 72 nM) and MEK2 (IC₅₀ = 58 nM). The inhibition is noncompetitive with respect to MEK substrates, ATP and ERK. Has very little effect on other kinases, such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. U0126 also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution™ format (Cat. No. 662009.
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	109511-58-2
Chemical formula	C₁₈H₁₆N₆S₂•½C₂H₅OH
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (200 mg/ml)
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Unstable in solution; reconstitute just prior to use.
Toxicity	Standard Handling
References	Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232. DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175. Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett. 8, 2839. Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.
Citation	Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun. 416, 232. Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953. Chengyu Wu and Jiaoti Huang. 2007. Journal of Biological Chemistry 282, 3571. Alexandra Thiel, Mira Heinonen, Johanna Rintahaka, Tuija Hallikainen, and Annabrita Hemmes, Dan A. Dixon, Caj Haglund, and Ari Ristimaki. (2006) EXPRESSION OF CYCLOOXYGENASE-2 IS REGULATED BY GSK-3 IN GASTRIC CANCER CELLS. Journal of Biological Chemistry in press,. Thiel, A., et al. 2006. Journal of Biological Chemistry 281, 4564. Basak, C., et al. 2005. Journal of Immunology 174, 5672. Soonkyu Chung, et al. (2005) Conjugated linoleic acid promotes human adipocyte insulin resistance through NF-κB-dependent cytokine production. Journal of Biological Chemistry 280, 38445-38456. Marie-Claire Delfini, et al. (2005) Control of the segmentation process by graded MAPK/ERK activation in the chick embryo. Proceedings of the National Academy of Science USA 102, 11343-11348. Gutzmer, R., et al. 2005. Journal of Immunology 5224. Monick, M.M., et al. 2005. Journal of Biological Chemistry 280, 2147. Tang, Q-Q., et al. 2005. Proceedings of the National Academy of Sciences (USA) 102, 9766. Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432. Wojciechowski, W., et al. 2005. Journal of Immunology 174, 7859. Wu, M-H., et al. 2005. The Journal of Clinical Endocrinology & Metabolism 90, 286. Yung-Luen Yu, et al. (2005) MAP kinase-mediated phosphorylation of GATA-1 promotes Bcl-XL expression and cell survival. Journal of Biological Chemistry 280, 29533-29542. Naoto Inukai, et al. (2004) A novel hydrogen peroxide-induced phosphorylation and ubiquitination pathway leading to RNA polymerase II proteolysis. Journal of Biological Chemistry 279, 8190-8195. Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385. Michael J. Cross, et al. (2002) The Shb Adaptor Protein Binds to Tyrosine 766 in the FGFR-1 and Regulates the Ras/MEK/MAPK Pathway via FRS2 Phosphorylation in Endothelial Cells. Molecular Biology of the Cell 13, 2881-2893.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > MAP Kinase Inhibitors

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