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Merck
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Key Documents

420097

Sigma-Aldrich

JAK Inhibitor I

InSolution, ≥98%

Synonym(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

Empirical Formula (Hill Notation):
C18H16FN3O
CAS Number:
457081-03-7
Molecular Weight:
309.34
MDL number:
MFCD17019334
UNSPSC Code:
12352200
NACRES:
NA.77

CN¥2,157.74

Available to ship onApril 24, 2025Details

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Quality Level

100

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

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

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Quality Level

100

Quality Level

200

Quality Level

-

Quality Level

-

mp

157-159 °C (lit.)

mp

−43 °C (lit.)

mp

157-159 °C (lit.)

mp

64-66 °C (lit.)

form

powder

form

liquid

form

-

form

-

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.

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

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

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class Code

10 - Combustible liquids

WGK

WGK 2

Flash Point(F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Flash Point(C)

87 °C - closed cup - (Dimethylsulfoxide)

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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
    JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes.
    Arnold, et al.
    International Journal of Molecular Sciences, 24 (2023)
    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
    Kirsty Ml Mackinlay et al.
    eLife, 10 (2021-08-18)
    Human embryogenesis entails complex signalling interactions between embryonic and extra-embryonic cells. However, how extra-embryonic cells direct morphogenesis within the human embryo remains largely unknown due to a lack of relevant stem cell models. Here, we have established conditions to differentiate
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