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420205 Sigma-AldrichHistone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem

Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures).

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

MSDS
分析证书
参考
技术信息
Data Sheet

同义词: GSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug

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价格及供货情况

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Description
Overview	A cell-permeable GSK-J1 (Cat. No. 420204) prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-α production in primary human macrophage cultures (IC₅₀ = 9 µM by ELISA). This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).
Catalogue Number	420205
Brand Family	Calbiochem®
Synonyms	GSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug

References
References	Heinemann, B., et al. 2014. Nature 514 E1. Kruidenier, L., et al. 2014. Nature 514, E2. Kruidenier, L., et al. 2012. Nature 488, 404.

Product Information
CAS number	1373423-53-0
Form	Tan semi-solid
Hill Formula	C₂₄H₂₇N₅O₂
Chemical formula	C₂₄H₂₇N₅O₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application	Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures).

Biological Information
Primary Target	H3K27me3 demethylases JMJD3 & UTX
Purity	≥98% 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). Stock solutions are stable for up to 6 months for -20°C.

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
420205-10MGCN	04055977210798

Documentation

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem 分析证书

标题	批号
420205	输入批号

参考

参考信息概述
Heinemann, B., et al. 2014. Nature 514 E1. Kruidenier, L., et al. 2014. Nature 514, E2. Kruidenier, L., et al. 2012. Nature 488, 404.

技术信息

标题
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics

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	06-September-2013 JSW
Synonyms	GSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug
Description	The H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]_t=0 = 30 µM; [cellular GSK-J1]_t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC₅₀ = 9 µM by ELISA), in primary human macrophage cultures.
Form	Tan semi-solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1373423-53-0
Chemical formula	C₂₄H₂₇N₅O₂
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.
Toxicity	Standard Handling
References	Heinemann, B., et al. 2014. Nature 514 E1. Kruidenier, L., et al. 2014. Nature 514, E2. Kruidenier, L., et al. 2012. Nature 488, 404.

种类

Life Science Research > Inhibitors and Biochemicals

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