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Merck

420097

JAK Inhibitor I

≥98% (HPLC), liquid

別名:

InSolution JAK Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, P6, Pyridone 6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X

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この商品について

実験式（ヒル表記法）:
C18H16FN3O
CAS番号:
457081-03-7
分子量:
309.34
MDL number:
MFCD17019334
UNSPSC Code:
12352200
NACRES:
NA.77

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製品名

JAK Inhibitor I, InSolution, ≥98%

SMILES string

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

assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

shipped in

wet ice

storage temp.

2-8°C

Quality Level

100

関連するカテゴリー

Biochem/physiol Actions

Cell permeable: yes
Primary Target
murine JAK1
Product competes with ATP.
Reversible: yes
Target IC50: 15 nM, 1 nM against murine JAK1 and JAK2, respectively; 1 nM against Tyk2
Target Ki: 5 nM against JAK3

Disclaimer

Toxicity: Irritant (B)

General description

A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). It inhibits other kinases only at much higher concentrations. Also inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks the phosphorylation of STAT5.

Other Notes

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

Packaging

Packaged under inert gas

Physical form

A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.

Preparation Note

Following initial use, aliquot and refrigerate (4°C).

Legal Information

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

保管分類

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

試験成績書（COA）

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文書ライブラリにアクセスする

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
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
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
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
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関連コンテンツ

PRODUCTO REGULADO POR LA SAGARPA
JAK/STAT Signaling Research Focus

The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.

CARTA DE USO GENERAL 2016

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PRODUCTO REGULADO POR LA SECRETARÍA DE SALUD

グローバルトレードアイテム番号

カタログ番号GTIN
420097-500UGCN04055977187861

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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