Cytokines play pivotal roles in immunity and inflammation, and targeting cytokines and their receptors is an effective means of treating such disorders. Type I and II cytokine receptors associate with Janus family kinases (JAKs; EC to effect intracellular signaling[1]. The JAK family in mammals consists of 4 members: JAK1, JAK2, JAK3 and TYK2. The unique structure of the JAK kinases clearly distinguishes them from other members of the protein tyrosine kinase family. The most intriguing feature of these proteins is the presence of two JAK-homology domains (JH1 and JH2), with extensive homology to the tyrosine kinase domains. A second interesting feature is the absence of any Src-homology domains SH2 or SH3. Instead, these proteins encode a group of well-conserved domains termed as JAK homology (JH1-JH7) domains that follow a non-conserved amino terminus of about 30-50 amino acids. Of the dual kinase domains identified, only the JH1 domain appears to be functional[2]. JAK activation occurs upon ligand-mediated receptor multimerization. The activated JAKs subsequently phosphorylate additional targets, including both the receptors and the major substrates, STATs (latent transcription factors that reside in the cytoplasm until activated)[3].

[1] M. Pesu et al. Therapeutic targeting of Janus kinases. Immunol. Rev. 2008, 223, 132-142.
[2] M.M. Seavey, P. Dobrzanski. The many faces of Janus kinase. Biochem. Pharmacol. 2012, 83, 1136-1145.
[3] J.S. Rawlings, K.M. Rosler, D.A. Harrison. The JAK/STAT signaling pathway. J. Cell. Sci. 2004, 117, 1281-1283.

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Axon ID Name Description From price
1378 AG 490 JAK2 inhibitor €65.00
3997 ASN-002 Potent dual inhibitor of SYK and pan-JAK kinases Inquire
2219 AT 9283 Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl) €85.00
1778 AZ 960 JAK2 inhibitor €95.00
3855 AZD-4205 Selective and ATP-competitive inhibitor of JAK1 Inquire
1955 Baricitinib Inhibitor of JAK1 and JAK2 €70.00
3813 BMS-911543 Potent, selective and orally active inhibitor of JAK2 Inquire
3671 CEP-33779 Potent, selective and orally bioavailable JAK2 inhibitor €95.00
2775 Cerdulatinib Orally active dual Syk/JAK inhibitor €85.00
1338 CP 690550 JAK3 inhibitor €60.00
3861 Decernotinib Potent and selective,orally bioavailable Janus kinase 3 (JAK3) inhibitor Inquire
4091 Deucravacitinib Potent, highly selective, allosteric and orally bioavailable TYK2 inhibitor €150.00
4006 GLPG-0634 The first orally-available, selective inhibitor of JAK1 Inquire
1843 JAK2 inhibitor 13 JAK2 inhibitor €110.00
2554 LY 2784544 Potent, selective and ATP-competitive inhibitor of mutated janus kinase 2 (JAK2V617F) €95.00
1681 Momelotinib JAK1 and JAK2 inhibitor €80.00
4124 Momelotinib hydrochloride JAK1 and JAK2 inhibitor €120.00
2792 NVP-BSK805 Potent, selective and orally bioavailable JAK2 inhibitor €125.00
3950 Peficitinib Potent and orally bioavailable JAK inhibitor €120.00
2217 PF 956980 JAK3 inhibitor; analogue of Axon 1338 and 2072 €90.00
1598 Ruxolitinib JAK1 and JAK2 inhibitor €65.00
2539 Solcitinib Selective JAK1 inhibitor for treatment of degenerative and inflammatory diseases €90.00
1588 TG 101348 JAK2 inhibitor €80.00
2072 Tofacitinib citrate Potent Janus Kinase 3 (JAK3) inhibitor €115.00
2316 WP 1066 Potent JAK2 and STAT3 inhibitor and downregulator of antiapoptotic proteins €95.00
2231 XL 019 JAK2 inhibitor €100.00

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