GSK-J5 (hydrochloride) - CAS:1797983-32-4

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GSK-J5 (hydrochloride)

目录号 : KCM12064 CAS No. : 1797983-32-4 纯度 : ≥95%

Data Sheet 产品使用指南

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 , an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base. However, the free base is a weak inhibitor of JMJD3 (IC > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock

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生物活性

GSK-J5 (hydrochloride) is a cell-permeable ester derivative of GSK J2, inactive. GSK-J5 hydrochloride is also an isomer of GSK-J4 and often used as a negative group.

体外研究

GSK-J5 (25 μM) has no effects at inhibiting the LPS-induced response of human primary macrophages derived from healthy volunteers. While GSK-J4 significantly reduced the expression of 16 of 34 LPS-driven cytokines as assessed by PCR array, such as TNF-α.
GSK-J5 (30 μM; 6 hours) is the inactive isomer of GSK-J4, has no effect on TNF-α protein production. But neither GSK-J4 nor GSK-J5 directly affects the levels of LPS-induced JMJD3 or of LPS-independent UTX and EZH2.
GSK-J5 (30 μM; 1 hour) can not prevent the LPS-induced loss of H3K27me3 associated with the TNFA TSS or block the recruitment of RNA polymerase II to this locus but GSK-J5 can. Finally, GSK-J4, but not GSK-J5, blocks the production of TNF-α by macrophages derived from patients with rheumatoid arthritis.

分子式

C₂₄H₂₇N₅O₂^.HCl

分子量

453.96

CAS号

1797983-32-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥95%

Data Sheet

产品使用指南

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

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工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器