GSK-J4,H3K27HistoneDemethylasesUTXandJMJD3Inhibitor M60063-2s|产品详情|进口橙子视频旧款采购网

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GSK-J4,H3K27HistoneDemethylasesUTXandJMJD3Inhibitor

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GSK-J4,H3K27HistoneDemethylasesUTXandJMJD3Inhibitor

品牌：Xcessbio

货号：M60063-2s

规格：2mg solid

货期：

应用：

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GSK-J4,H3K27HistoneDemethylasesUTXandJMJD3Inhibitor

商品详情参考文献相关资料

Product Information

Molecular Weight:	417.50
Formula:	C₂₄H₂₇N₅O₂
Purity:	≥98%
CAS#:	1373423-53-0
Solubility:	DMSO up to 100 mM
Chemical Name:	ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate
Storage:	Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Biological Activity:

GSK-J4 is an ethyl ester derivative of GSK-J1, which is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. The highly polar carboxylate group of GSK-J1 restricts its cellular permeability, therefore GSK-J4 was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays. GSK-J4 could significant reduce LPS-induced pro-inflammatory cytokine production in primary human macrophages (IC₅₀ ~9 μM for the inhibition of TNFα release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.

How to Use:

In vitro: GSK-J4 was used at 30 µM final concentration in cellular assays.
In vivo: n/a

Reference:

1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response (2012) Nature. 488(7411):404-8.
2. SGC website: http://www.thesgc.org/scientists/chemical_probes/GSKJ1

Products are for research use only. Not for human use.

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