AT9283 is a multitargeted kinase inhibitor which potently inhibits aurora kinase A/B, JAK2/3 (IC50=1.2 nM, 1.1 nM).
JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively. JAK3-IN-14 shows inhibitory of IL-4 and IL-3 induced TF-1 cell proliferation, with IC50 values of 600 and 500 nM, respectively[1].
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively[1].
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain[1][2].
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].
JAK-2/3-IN-2 (Compound 3h) is a JAK2 and JAK3 inhibitor with IC50s of 23.85 nM and 18.9 nM, respectively[1].
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1)[1].
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL)[1].
JAK3-IN-12 (compound 15k) is a highly potent JAK3 inhibitor with an IC50 value of 9.5 nM. JAK3-IN-12 can be used for researching rheumatoid arthritis[1].
Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871[1].
Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).
Rovadicitinib is a Janus kinase (JAK) inhibitor with an IC50 value <20 nM. Rovadicitinib also exhibits anti-inflammatory activity[1][2].
JAK3/BTK-IN-1 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002)[1].
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively[1][2].
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM[1].
JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC50 values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED)[1].
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells[1].
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3.
TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research[1].
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
JAK-STAT-IN-1 (compound 1) is a selective JAK-STAT inhibitor. JAK-STAT-IN-1 can be used for the research of autoimmune disorder[1].
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo[1].
JAK3/BTK-IN-2 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)[1]
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model[1].
AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
Zotiraciclib (TG02) is an orally active potent inhibitor of CDK2, JAK2 and FLT3 with IC50 values of 13, 73, and 56 nM, respectively. Zotiraciclib can be used for the research of advanced leukemias and multiple myeloma[1][2].
Ifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib can be used in studies of allergies, asthma and autoimmune diseases[1].
PF-06700841 P-Tosylate is a dual JAK1 and TYK2 inhibitor with IC50s of 17 and 23 nM, respectively. Anti-inflammatory activity[1].
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].