JAK Inhibitor I CAS: 457081-03-7
MF: C18H16FN3O
MW: 309.34
An inhibitor of JAK1, JAK2, and JAK3.

JAK Inhibitor I (CAS 457081-03-7)

JAK Inhibitor I | CAS 457081-03-7 is rated 5.0 out of 5 by 1.
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Synonym: Pyridone 6; 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
Application: An inhibitor of JAK1, JAK2, and JAK3
CAS Number: 457081-03-7
Purity: ≥98%
Molecular Weight: 309.34
Molecular Formula: C18H16FN3O
* Refer to Certificate of Analysis for lot specific data (including water content).
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JAK Inhibitor I is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1, JAK2, and JAK3. Primary target: murine JAK1. JAK1 (Janus kinase 1), JAK2 and JAK3 belong to the family of non-receptor janus tyrosine kinases, which regulate a spectrum of cellular functions downstream of activated cytokine receptors in the lympho-hematopoietic system. Immunological stimuli, such as interferons and cytokines, induce recruitment of STAT transcription factors to cytokine receptor-associated JAK1, JAK2 and JAK3.


1. Chi, X. and Tai, H.H. 2010. Exp. Cell Res. PMID: 20685602
2. Chrencik, J.E. et al. 2010. J. Mol. Biol. 400(3): 413-433. PMID: 20478313
3. Taura, M. et al. 2010. Cancer Sci. 101(7): 1610-1617. PMID: 20367642
4. Matsunaga, Y. et al. 2011. Biochem. Biophys. Res. Commun. 404(1): 261-267. PMID: 21111712
5. Nakagawa, R. et al. 2011. J. Immunol. 187(9): 4611-4620. PMID: 21957150

Physical State :
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at -20° C
Melting Point :
251.66° C (Predicted)
Boiling Point :
646.48° C at 760 mmHg (Predicted)
Density :
1.33 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
JAK2: IC50 = 1 nM; Tyk2: IC50 = 1 nM; Fer: IC50 = 1 nM (human); JAK1: IC50 = 15 nM (mouse); JAK3: IC50 = 5 nM (human)
Ki Data :
ZIP-kinase: Ki= 1 nM (human); JNK1: Ki= 15.85 nM (human); JAK2: Ki= 2.51 nM (human); LTK: Ki= 25.12 nM (human); JAK3: Ki= 5 nM
pK Values :
pKa: 11.77 (Predicted), pKb: 7.19 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :

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Certificate of Analysis

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JAK Inhibitor I  Product Citations

See how others have used JAK Inhibitor I. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 36 total

PMID: # 30632069  Yin, X.|Zhang, S.|Li, B.|Zhang, Y.|Zhang, X.| et al. 2019. Mol. Biol. Rep. 46: 1189-1197.

PMID: # 29981150  Sun, W.|Liao, Y.|Yi, Q.|Wu, S.|Tang, L.|Tong, L.| et al. 2018. Photochem. Photobiol. 94: 1234-1239.

PMID: # 29160908  Rayego-Mateos, S.|Morgado-Pascual, JL.|Rodrigues-Diez, RR.|Rodrigues-Diez, R.|Falke, LL.|Mezzano, S.|Ortiz, A.|Egido, J.|Goldschmeding, R.|Ruiz-Ortega, M.| et al. 2018. J. Pathol. 244: 227-241.

PMID: # 28447667  Fernández-Laso, V. et al. 2017. Sci Rep. 7: 46679.

PMID: # 29019987  Yang, J.|Ryan, DJ.|Wang, W.|Tsang, JC.|Lan, G.|Masaki, H.|Gao, X.|Antunes, L.|Yu, Y.|Zhu, Z.|Wang, J.|Kolodziejczyk, AA.|Campos, LS.|Wang, C.|Yang, F.|Zhong, Z.|Fu, B.|Eckersley-Maslin, MA.|Woods, M.|Tanaka, Y.|Chen, X.|Wilkinson, AC.|Bussell, J.|White, J.|Ramirez-Solis, R.|Reik, W.|Göttgens, B.|Teichmann, SA.|Tam, PPL.|Nakauchi, H.|Zou, X.|Lu, L.|Liu, P.| et al. 2017. Nature. 550: 393-397.

PMID: # 28864784  Seo, HS. et al. 2017. Biosci. Rep.

PMID: # 28383550  Wassermann-Dozorets, R. et al. 2017. Cell Death Dis. 8: e2733.

PMID: # 28656316  Seo, HS. et al. 2017. Oncol. Rep. 38: 715-724.

PMID: # 28077314  Wang, W. et al. 2017. Antiviral Res. 140: 1-12.

PMID: # 27328944  Xu, L. et al. 2016. FASEB J. 30: 3352-3367.

Citations 1 to 10 of 36 total

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Answered by: Technical Support Europe
Date published: 2017-07-14
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Rated 5 out of 5 by from Taura Taura, M. et al. (PubMed 20367642) used product sc-204021 (JAK Inhibitor I) to determine if TLR3 up-regulation by IFN-alpha is mediated by the JAK/STAT pathway. Found that inhibition of JAK/STAT pathway blocked the IFN-alpha up-regulation of TLR3. -SCBT Publication Review
Date published: 2015-03-16
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