jak3

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3 2 1 (IC50=1 20 112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1 2 3 (IC50s: 1 20 112 nM).

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1 2) with IC50 of 11 nM 18 nM. JAK1 2 inhibitor CYT387 competes with JAK1 2 for ATP binding, which may result in inhibition of JAK1 2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1 2-expressing tumor cells.

Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23 22 nM, in cell-free assays).

Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, including the drug-resistant T790M EGFR mutant, which prevents signaling mediated by mutant forms of EGFR. This may both induce cell death and inhibit tumor growth in EGFR-mutated tumor cells. EGFR, a receptor tyrosine kinase that is mutated in a variety of Ys, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.

TG101209 is a selective JAK2 inhibitor with an IC50 of 6 nM.

Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.

JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a JAK1 3 inhibitor with pIC50 of 4.4 7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1 JAK2 inhibitor.

TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.

ZM39923 hydrochloride (JAK3 Inhibitor IV) is an JAK1 3 inhibitor with pIC50 of 4.4 7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

JAK3 BTk-in-2 is a potent JAK3 BTK inhibitor. JAK3 BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3 BTk-in-2 simultaneously inhibits the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) intended for the treatment of organ transplantation rejection, graft-versus-host reaction post-transplantation, autoimmune disorders, allergic diseases, and chronic myeloproliferative disorders.

JAK3 BTk-in-1 is a dual JAK3 BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3 BTk-in-1 simultaneously inhibited the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.