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JAK

Janus kinases (JAKs) are non-receptor tyrosine kinases which play the key role in JAK-STAT signaling pathway. A large number of cytokines depend on JAK including interleukin (IL)-2, IL-4, IL-7, IL-9, IL-15 and IL-21. Jak kinases are involved in malignant cell growth and survival. Jak kinases have been shown to modulate activation of Ras-Raf-MAP kinase pathways which are implicated in malignant transformation. The function of Jak kinases is also related to Abl. Jak kinases have been also implicated in the regulation of p53-dependent cell-cycle arrest and apoptosis, for example, Jak kinases can regulate the levels of Bcl-XL, Bcl-2 and Bax expression by their effects on Stats and other receptor linked pathways such as the PI-3 kinase and the Ras-MAPK pathways.

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S5001 Tofacitinib citrate (CP-690550 citrate) Tofacitinib citrate (CP-690550) is a potent JAK3 inhibitor with IC50 of 1 nM. (5)
S2736 TG101348 (SAR302503) TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM.
S2789 Tofacitinib (CP-690550, Tasocitinib) CP-690550 is a novel inhibitor of JAK3 with IC50 of 1 nM. (11)
S2162 AZD1480 AZD1480 is a novel ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 1.3 nM and 0.26 nM, respectively. (1)
S1143 AG-490 AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively. (2)
S2219 Cyt387 CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 nM and 18 nM, respectively. (1)
S2686 NVP-BSK805 NVP-BSK805 is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM.
S8004 ZM 39923 HCl ZM39923 is an JAK inhibitor for JAK1, JAK3, EFGR and TGM2 with IC50 of 4.4 μM, 7.1 μM, 5.6 μM and 10 nM, respectively.
S2867 WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM and also inhibits EGFR with IC50 of 4 nM.
S2851 Baricitinib (LY3009104, INCB28050) Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells .

JAK

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