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CAS No.: 1443235-95-7

JAK3-IN-6 Catalog No. CSN23767

Synonyms: JAK3-IN-2

JAK3-IN-6 is an irreversible, potent and highly selective JAK3 inhibitor with IC50 value of 0.15 nM, 4300-fold selective for JAK3 over JAK1 in enzyme assays.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述JAK3-IN-6 is an irreversible, potent and highly selective JAK3 inhibitor with IC50 value of 0.15 nM, 4300-fold selective for JAK3 over JAK1 in enzyme assays. JAK3-IN-6 blocked the cytokine signaling through selective inhibition of JAK3 but not other JAK family enzymes. Inhibition of JAK3 by JAK3-IN-6 led inhibition of IL-2 signaling (70nM), inhibition of IL-7-induced pSTAT5 in CD31 and CD81 T cells from human PBMCs (IC50=280nM), but inhibited GMCSF-induced pSTAT5 in CD141 monocytes from human PBMCs with an IC50 value up to 9600 nM. JAK3-IN-6 inhibited IL-7, IL-15, and IL-2 signaling in T cells. Administration of JAK3-IN-6 resulted inhibition of paw swelling of a collagen induced-arthritis model by 58%, 92% and 96%, with inhibition of bone loss in the ankle, at dose of 100, 300 and 600mg/kg. The reduction of paw swelling and joint degradation and inhibition of leukocyte proliferation can also observed.
作用机制JAK3-IN-6 can generate a covalent protein-inhibitor bond with the JAK3 protein through JAK3 cysteine residues.^[1]
参考文献

[1] Elwood F, Witter DJ, et al. Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor. J Pharmacol Exp Ther. 2017 May;361(2):229-244.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8541 mL
- 14.2706 mL
- 28.5413 mL
- 5 mM
- 0.5708 mL
- 2.8541 mL
- 5.7083 mL
- 10 mM
- 0.2854 mL
- 1.4271 mL
- 2.8541 mL

技术信息

CAS号

1443235-95-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18N4O3

运输

蓝冰

分子量

350.37

别名

JAK3-IN-2

溶解度

DMSO	60.0 mg/mL (171.2 mM)
Water	13.5 mg/mL (38.5 mM)

动物实验配方

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