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203290 Sigma-AldrichBisindolylmaleimide I - CAS 133052-90-1 - Calbiochem

Bisindolylmaleimide I, CAS 133052-90-1, is a cell-permeable, highly selective, reversible inhibitor of protein kinase C (IC50 = 10 nM). Acts on the ATP-binding site of PKC.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet
Citations

同义词: 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, GF 109203X, Gö 6850

Primary Target: PKC

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
133052-90-1	C₂₅H₂₄N₄O₂

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
203290-1MGCN	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	塑胶安瓿;塑胶针药瓶	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
203290-250UGCN	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	250 μg	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 highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC₅₀ = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα-, β_I-, β_II-, γ-, δ-, and ε- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC₅₀ = 360 nM) and in GSK-3β immunoprecipitates (IC₅₀ = 170 nM). May inhibit protein kinase A at a much higher concentration (IC₅₀ = 2 µM). A 1 mg/ml solution of Bisindolylmaleimide I (Cat. No. 203293) in anhydrous DMSO is also available.
Catalogue Number	203290
Brand Family	Calbiochem®
Synonyms	2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, GF 109203X, Gö 6850

References
References	Hers, I., et al. 1999. FEBS Lett. 460, 433. Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730. Gekeler, V., et al. 1996. Br. J. Cancer 74, 897. Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93. Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.

Product Information
CAS number	133052-90-1
ATP Competitive	Y
Form	Deep orange solid
Hill Formula	C₂₅H₂₄N₄O₂
Chemical formula	C₂₅H₂₄N₄O₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application	Bisindolylmaleimide I, CAS 133052-90-1, is a cell-permeable, highly selective, reversible inhibitor of protein kinase C (IC50 = 10 nM). Acts on the ATP-binding site of PKC.

Biological Information
Primary Target	PKC
Primary Target IC<sub>50</sub>	10 nM against protein kinase C (PKC); 360 nM, 170 nM against GSK-3 in primary adipocyte lysates and in GSK-3β immunoprecipitates, respectively
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

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	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.

Packaging Information

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
203290-1MGCN	04055977221121
203290-250UGCN	07790788048327

Documentation

Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem 分析证书

标题	批号
203290	输入批号

参考

参考信息概述
Hers, I., et al. 1999. FEBS Lett. 460, 433. Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730. Gekeler, V., et al. 1996. Br. J. Cancer 74, 897. Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93. Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.

引用

标题

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,.

Xiaohua Jiang, et al. (2005) Hyperhomocystinemia impairs endothelial function and eNOS activity via PKC activation. Arteriosclerosis, Thrombosis, and Vascular Biology in press,.

Ademi E. Santiago-Walker, et al. (2005) Protein Kinase C δ Stimulates Apoptosis by Initiating G1 Phase Cell Cycle Progression and S Phase Arrest. Journal of Biological Chemistry 280, 32107-32114.

Wojciech Wojciechowski, et al. (2005) Enhanced Expression of CD20 in Human Tumor B Cells is Controlled Through ERK-Dependent Mechanisms. Journal of Immunology 174, 7859-7868.

Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.

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	05-May-2010 RFH
Synonyms	2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide, GF 109203X, Gö 6850
Description	A highly selective cell-permeable protein kinase C (PKC) inhibitor (IC₅₀ = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα, β_I, β_II, γ, δ, and ε isozymes. May inhibit protein kinase A at a much higher concentration (IC₅₀ = 2 µM). Also inhibits telomerase activity in quercetin, H-89, or herbimycin A treated NPC-076 cells.
Form	Deep orange solid
CAS number	133052-90-1
Chemical formula	C₂₅H₂₄N₄O₂
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (10 mg/ml). Further dilute with aqueous buffers just prior to use.
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
Toxicity	Standard Handling
References	Hers, I., et al. 1999. FEBS Lett. 460, 433. Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730. Gekeler, V., et al. 1996. Br. J. Cancer 74, 897. Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93. Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.
Citation	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,. Xiaohua Jiang, et al. (2005) Hyperhomocystinemia impairs endothelial function and eNOS activity via PKC activation. Arteriosclerosis, Thrombosis, and Vascular Biology in press,. Ademi E. Santiago-Walker, et al. (2005) Protein Kinase C δ Stimulates Apoptosis by Initiating G1 Phase Cell Cycle Progression and S Phase Arrest. Journal of Biological Chemistry 280, 32107-32114. Wojciech Wojciechowski, et al. (2005) Enhanced Expression of CD20 in Human Tumor B Cells is Controlled Through ERK-Dependent Mechanisms. Journal of Immunology 174, 7859-7868. Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618. 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 > Protein Kinase C (PKC) Inhibitors

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