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Merck
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420097

Sigma-Aldrich

JAK Inhibitor I

InSolution, ≥98%

Sinônimo(s):

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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About This Item

Fórmula empírica (Notação de Hill):
C18H16FN3O
Número CAS:
Peso molecular:
309.34
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

liquid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
desiccated (hygroscopic)
protect from light

Condições de expedição

wet ice

temperatura de armazenamento

2-8°C

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)

chave InChI

VNDWQCSOSCCWIP-UHFFFAOYSA-N

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

forma física

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

Reconstituição

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

Outras notas

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

Informações legais

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

Código de classe de armazenamento

10 - Combustible liquids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Ponto de fulgor (°C)

87 °C - closed cup - (Dimethylsulfoxide)


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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
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes.
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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
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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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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