GSK-J4 hydrochloride|cas:1797983-09-5|西域试剂

GSK-J4 hydrochloride,98.83%

产品编号：Bellancom-15648F| CAS NO：1797983-09-5| 分子式：C₂₄H₂₈ClN₅O₂| 分子量：453.96

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-15648F		￥1200.00	杭州北京（现货）
Bellancom-15648F		￥4500.00	杭州北京（现货）

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GSK-J4 hydrochloride

产品介绍

GSK-J4 hydrochloride 是一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC₅₀ 分别为 8.6 μM 和 6.6 μM。GSK-J4 hydrochloride 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC₅₀ 值为 9 μM。GSK-J4 hydrochloride 是 GSK-J1 的细胞通透性前体。

生物活性

GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1.

体外研究

GSK-J4 Hydrochloride has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α).
GSK-J4 Hydrochloride (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels.
GSK-J4 Hydrochloride (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells.
GSK-J4 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1^[4].
GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.
GSK-J4 Hydrochloride (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Eight-week-old male db/m and db/db mice on a BKS background
Dosage:	10 mg/kg
Administration:	i.p.; thrice-weekly for 10 weeks
Result:	Attenuated the development of kidney disease in diabetic mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Eight-week-old male db/m and db/db mice on a BKS background
Dosage:	10 mg/kg
Administration:	i.p.; thrice-weekly for 10 weeks
Result:	Attenuated the development of kidney disease in diabetic mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (137.68 mM; Need ultrasonic)

H₂O : 3.33 mg/mL (7.34 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2028 mL	11.0142 mL	22.0284 mL
5 mM	0.4406 mL	2.2028 mL	4.4057 mL
10 mM	0.2203 mL	1.1014 mL	2.2028 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明