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JAK inhibitors

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.

Other JAK/STAT Related Inhibitors

STAT Pim

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1378 Ruxolitinib (INCB18424) Ruxolitinib (INCB18424) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. This compound kills tumor cells through toxic mitophagy. It induces autophagy and enhances apoptosis.
Nature, 2025, 10.1038/s41586-025-08938-8
Nat Commun, 2025, 16(1):8409
Nat Commun, 2025, 16(1):492
Verified customer review of Ruxolitinib (INCB18424)
S5001 CP-690550 (Tofacitinib) Citrate Tofacitinib citrate (CP-690550, Tasocitinib) is a novel JAK inhibitor with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. It also has anti-infection activity.
Cells, 2025, 14(2)102
Front Pharmacol, 2025, 16:1549183
J Exp Clin Cancer Res, 2024, 43(1):64
Verified customer review of CP-690550 (Tofacitinib) Citrate
S5243 Ruxolitinib (INCB18424) Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Nat Commun, 2024, 15(1):10718
Cell Mol Life Sci, 2024, 82(1):14
Virol J, 2024, 21(1):23
S2851 Baricitinib (LY3009104) Baricitinib (LY3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. It is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Cell Rep Med, 2025, 6(3):102027
Cell Rep, 2025, 44(3):115403
Cell Rep, 2025, S2211-1247(25)00781-8
Verified customer review of Baricitinib (LY3009104)
S8162 ABT-494 (Upadacitinib) Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.
J Crohns Colitis, 2025, 19(6)jjaf076
J Crohns Colitis, 2025, 19(6)jjaf076
Nature, 2024,
S8879 BMS-986165 (Deucravacitinib) Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.
Res Sq, 2025, rs.3.rs-6079043
Nat Commun, 2024, 15(1):1718
Nat Commun, 2024, 15(1):1337
S2789 Tofacitinib (CP-690550) Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. This compound inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.
Cell Rep Med, 2025, S2666-3791(25)00102-8
EMBO Mol Med, 2025, 10.1038/s44321-025-00317-0
J Crohns Colitis, 2025, 19(6)jjaf076
Verified customer review of Tofacitinib (CP-690550)
S2162 AZD1480 AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
Int J Biol Sci, 2025, 21(1):271-284
Biochem Pharmacol, 2025, 242(Pt 2):117306
Sci Adv, 2025, 11(4):eadq2395
Verified customer review of AZD1480
S2736 Fedratinib (TG101348) Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
Leukemia, 2025, 39(7):1678-1691
Front Immunol, 2025, 16:1514618
Cancer Immunol Immunother, 2025, 74(3):79
Verified customer review of Fedratinib (TG101348)
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.
Cancer Med, 2025, 14(18):e71239
Nat Commun, 2024, 15(1):1987
Cancer Cell Int, 2024, 24(1):60
Verified customer review of WP1066

Signaling Pathway Map