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Merck
CN
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主要文件

420097

Sigma-Aldrich

Janus蛋白酪氨酸激酶(JAK)抑制剂I

InSolution, ≥98%

别名:

InSolution JAK抑制剂I, 2-（1，1-二甲基乙基）-9-氟-3，6-二氢-7H-苯并[h]-咪唑[4，5-f]异喹啉-7-酮，P6，吡啶酮6，DBI，JAK1抑制剂I，JAK2抑制剂I，JAK3抑制剂X

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About This Item

经验公式（希尔记法）:
C18H16FN3O
CAS号:
457081-03-7
分子量:
309.34
MDL编号:
MFCD17019334
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

liquid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

运输

wet ice

储存温度

2-8°C

SMILES字符串

Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1

InChI

1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)

InChI key

VNDWQCSOSCCWIP-UHFFFAOYSA-N

一般描述

Janus蛋白酪氨酸激酶（JAKs）的有效抑制剂。显示对JAK1（对于鼠JAK1，IC50=15 nM）、JAK2（IC50=1 nM）、JAK3（Ki=5 nM）和Tyk2（IC50=1 nM）的有效抑制活性。它仅在高得多的浓度下抑制其他激酶。还抑制CTLL细胞的IL-2和IL-4依赖性增殖，并阻断STAT5的磷酸化。

生化/生理作用

5 nM，针对JAK3
主要靶标
鼠JAK1
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：分别针对鼠JAK1和JAK2的15 nM，1 nM；针对Tyk2为1 nM

包装

用惰性气体包装

警告

毒性：刺激性（B）

外形

10 mM（500 µg/162 µl）JAK抑制剂I（目录号420099）的DMSO溶液。

重悬

初次使用后，等分并冷藏（4°C）。

其他说明

Thompson, J.E., et al. 2002.Bioorg.Med. Chem. Lett.12, 1219.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

10 - Combustible liquids

WGK

WGK 2

闪点(°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

闪点(°C)

87 °C - closed cup - (Dimethylsulfoxide)

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JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes.
Arnold, et al.
International Journal of Molecular Sciences, 24 (2023)
Feras M Ghazawi et al.
Immunology and cell biology, 91(2), 149-158 (2012-12-05)
Interleukin (IL)-7 is an essential nonredundant cytokine, and throughout the lifespan of a T-cell signaling via the IL-7 receptor influences cell survival, proliferation and differentiation. It is therefore no surprise that expression of the IL-7 receptor alpha-chain (CD127) is tightly
Julia Ettich et al.
The Journal of biological chemistry, 299(11), 105270-105270 (2023-09-22)
Synthetic cytokine receptors can modulate cellular functions based on an artificial ligand to avoid off-target and/or unspecific effects. However, ligands that can modulate receptor activity so far have not been used clinically because of unknown toxicity and immunity against the
Sandra March et al.
Nature protocols, 10(12), 2027-2053 (2015-11-20)
The development of therapies and vaccines for human hepatropic pathogens requires robust model systems that enable the study of host-pathogen interactions. However, in vitro liver models of infection typically use either hepatoma cell lines that exhibit aberrant physiology or primary
Kathryn G V Anderson et al.
Nature cell biology, 19(10), 1164-1177 (2017-09-26)
Signalling downstream of Activin/Nodal (ActA) and Wnt can induce endoderm differentiation and also support self-renewal in pluripotent cells. Here we find that these apparently contradictory activities are fine-tuned by insulin. In the absence of insulin, the combination of these cytokines
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