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重要文件

420097

Sigma-Aldrich

Janus蛋白酪氨酸激酶(JAK)抑制剂I

InSolution, ≥98%

同義詞:

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

經驗公式(希爾表示法):
C18H16FN3O
CAS號碼:
分子量::
309.34
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77
暫時無法取得訂價和供貨情況

品質等級

化驗

≥98% (HPLC)

形狀

liquid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
desiccated (hygroscopic)
protect from light

運輸包裝

wet ice

儲存溫度

2-8°C

SMILES 字串

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 密鑰

VNDWQCSOSCCWIP-UHFFFAOYSA-N

一般說明

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

包裝

用惰性气体包装

警告

毒性:刺激性(B)

外觀

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

重構

初次使用后,等分并冷藏(4°C)。

其他說明

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

法律資訊

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

儲存類別代碼

10 - Combustible liquids

水污染物質分類(WGK)

WGK 2

閃點(°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

閃點(°C)

87 °C - closed cup - (Dimethylsulfoxide)


分析證明 (COA)

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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
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes.
Arnold, et al.
International Journal of Molecular Sciences, 24 (2023)
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

Questions

  1. Can the InSolution JAK Inhibitor I - CAS 457081-03-7 - Calbiochem also target human JAK, considering that its primary target is stated as murine? I am in search of an inhibitor for human JAK.

    1 answer
    1. Our laboratory has not validated this product for use on human JAK. However, based on the provided citation, the inhibitor appears to demonstrate effective activity on human cells as well. The study titled "Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor" published in Int J Oncol. 2018 Oct;53(4):1681-1690 (PMID: 30066853) supports this observation.

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