jak3i

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.

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.

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.

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

WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor.

JAK3-IN-15 (compound 22) is a JAK3 inhibitor that reduces the secretion of p-JAK3 induced by LPS. It is utilized in research for rheumatoid arthritis.

JANEX-1 (Jak3 inhibitor I) is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Syk or SRC tyrosine kinases.

JAK3-IN-16 (compound 6) is a covalent inhibitor of JAK3.

JAK3-IN-17 is an orally active JAK3 inhibitor with an IC50 of 14.56 nM. It demonstrates anti-inflammatory activity by inhibiting the production of IL-2 and IL-6 in a DNCB-induced mouse model of atopic dermatitis.

JAK3-IN-18 is a selective and orally active dual inhibitor targeting JAK3 and TEC, with IC50 values of 0.5391 nM and 12.40 nM, respectively. It demonstrates remarkable selectivity for AK1, AK2, and TYK2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 exhibits exceptional therapeutic efficacy in a mouse model of experimental autoimmune encephalomyelitis and is applicable for multiple sclerosis research.

JAK3-IN-19 (Compound 4) is an inhibitor of JAK3 and can be used for cancer research.

JAK3-IN-20 is an orally active, selective JAK3 inhibitor with an IC50 of 0.7473 nM. It forms a covalent bond with JAK3Cys909 and competitively occupies the ATP catalytic site, blocking activation of the JAK-STAT pathway. JAK3-IN-20 effectively inhibits migration, proliferation, and tumor growth in Bortezomib-resistant cancer cells, and induces dose-dependent apoptosis (apoptosis). It is applicable for research on Bortezomib-resistant multiple myeloma.

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.

JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM

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-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].

JAK3-IN-12 (compound 15k) is a potent inhibitor of JAK3 (IC50: 9.5 nM) and can be used in the study of rheumatoid arthritis.

JAK3-IN-13 is a potent, selective, orally active JAK3 inhibitor with IC50 values of 4728 nM for NK1, 2039 nM for JNK2, 8 nM for JNK3, and 365 nM for Tyk2. JAK3-IN-13 also exhibits anti-tumor effects.

JANEX-1 (WHI-P131) hydrochloride is an effective and specific JAK3 inhibitor with a Ki of 2.3 μM and an IC50 of 78 μM. It does not inhibit JAK1 and JAK2.