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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Alternate Names: Pyridone 6; 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
Application: JAK Inhibitor I is an inhibitor of JAK1, JAK2, and JAK3
CAS Number: 457081-03-7
Purity: ≥98%
Molecular Weight: 309.34
Molecular Formula: C18H16FN3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* 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.


References

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 :
Solid
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 :
MFCD17019334
SMILES :
CC(C)(C)C1=NC2=C(N1)C3=C(C=C(C=C3)F)C4=C2C=CNC4=O

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Certificate of Analysis

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JAK Inhibitor I (CAS 457081-03-7)  Product Citations

See how others have used JAK Inhibitor I (CAS 457081-03-7). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 52 total

PMID: # 33692219  Sun, Y.|Jing, J.|Xu, H.|Xu, L.|Hu, H.|Tang, C.|Liu, S.|Wei, Q.|Duan, R.|Guo, J.|Yang, L.| et al. 2021. J Immunother Cancer. 9:

PMID: # 34157403  Miao, Z.|Zhang, R.|Yu, P.|Li, Y.|Pan, Q.|Li, Y.| et al. 2021. Int J Antimicrob Agents. 106383.

PMID: # 32452409  Yu, P.|Li, Y.|Wang, Y.|Peppelenbosch, MP.|Pan, Q.| et al. 2020. Virology. 546: 109-121.

PMID: # 32432721  Pozzi, B.|Bragado, L.|Mammi, P.|Torti, MF.|Gaioli, N.|Gebhard, LG.|García Solá, ME.|Vaz-Drago, R.|Iglesias, NG.|García, CC.|Gamarnik, AV.|Srebrow, A.| et al. 2020. Nucleic Acids Res.

PMID: # 31901521  Gibbs, KD.|Washington, EJ.|Jaslow, SL.|Bourgeois, JS.|Foster, MW.|Guo, R.|Brennan, RG.|Ko, DC.| et al. 2020. Cell Host Microbe. 27: 129-139.e4.

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

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

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.

Citations 1 to 10 of 52 total

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Estimado cliente, Muchas gracias por su mensaje. La mayoría de los productos se encuentran disponibles en nuestra sede Europea y pueden ser enviados dentro de un día si recibimos su pedido antes de las 17.30 (Horario Central Europeo). Si desea recibir un plazo de entrega más específico, por favor solicite un presupuesto contactando a nuestro soporte técnico por teléfono, correo electrónico o chat.
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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