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420097

JAK Inhibitor I

Name: JAK Inhibitor I
Brand: MM

≥98% (HPLC), liquid

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

Assay:

≥98% (HPLC)

Form:

liquid

Quality level:

100

Storage condition:

OK to freeze, desiccated (hygroscopic), protect from light

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Properties

Product Name

JAK Inhibitor I, InSolution, ≥98%

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

Description

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 (K_i = 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 K_i: 5 nM against JAK3

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).

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

Disclaimer

Toxicity: Irritant (B)

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Storage Class

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

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