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.

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

JAK-IN-10 is a JAK inhibitor. JAK-IN-10 can be used for the research of dry eye disorders.

JAK-IN-5 is a JAK inhibitor.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

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/ 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.

JAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.

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.

JAK-IN-5 hydrochloride is a JAK inhibitor [1].

JAK2/STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

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.

JAK-2/3-IN-1 is a highly effective inhibitor targeting both JAK-2 and JAK-3 isoforms. It exhibits remarkable potency, with Ki values below 250 nM for both isoforms.

JAK2-IN-6, a polysubstituted aminothiazole derivative, is a potent and selective inhibitor of JAK2 (ic50 at 22.86 μg/mL). Jak2-in-6 inhibits the activity of JAK2 enzymes by interfering with Jak2-related signaling pathways, thereby producing therapeutic effects on the specific disease IN which JAK2 is dysregulated, and does not show activity on JAK1 and JAK3. JAK2 is a protein involved in signaling pathways that regulate cell growth and division. Abnormal activation of JAK2 has been linked to a variety of diseases, including some types of cancer and inflammatory diseases. JAK2-IN-6 has antiproliferative activity against cancer cells.

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3, and 1.95 nM for TYK2. It effectively reduces joint swelling while maintaining a good safety profile [1].

JAK-IN-33 (Compound 3 (R)) is a selective inhibitor of the Janus kinase (JAK) family [1].

Tubulin/JAK2-IN-1 (compound 7g) serves as a potent dual inhibitor targeting both Janus kinase 2 (JAK2) and microtubules, demonstrating significant antiproliferative effects against cancer cells [1].

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. Moreover, JAK-IN-27 impedes IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells with an IC50 of 23.7 nM [1].

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4. This compound not only inhibits cell proliferation but also induces apoptosis in MDA-MB-231 cells and demonstrates in vivo anticancer efficacy [1].

JAK-IN-15 is a JAK inhibitor. WO2016119700A1 (Compound 15).

JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC 50 of <5 μM. JAK-IN-14 is more than 8-fold selective for JAK1 than JAK2 and JAK3 [1].

JAK-IN-26 (compound 2) is an orally active inhibitor of the Janus kinase (JAK) enzyme with favorable pharmacokinetic properties, exhibiting potency in suppressing IFN-α2B-induced STAT3 phosphorylation in Jurkat cells with an IC50 value of 17.2 nM [1].

JAK-IN-28 (Compound 111) is a Janus kinase (JAK) inhibitor potentially applicable in the research of cancer and inflammatory diseases [1].

JAK-IN-19 is a potent inhibitor of JAK, with pIC50 values of 7.2 and 7.7 for PBMC IFNγ and HLF Eotaxin, respectively. The pIC50 values for VEGFR2 and Aurora B are 7.0 and 5.8 respectively).

JAK2 Inhibitor V (JAK2 Inhibitor V Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.

JAK-IN-18 is a potent inhibitor of JAK and can be used to study a variety of diseases, particularly eye, skin and respiratory diseases.

JAK-IN-25 (compound 19), a potent JAK inhibitor, exhibits IC50 values of 6 nM for TYK2, 21 nM for JAK1, 8 nM for JAK2, and 1051 nM for JAK3. It also demonstrates an IC50 of 28 nM against human whole blood IL-12 (HEB IL-12) and holds potential for cancer research [1].

JAK-IN-31 (Example 75), a JAK inhibitor, demonstrates IC50 values of ≤0.01 µM for JAK1, ≤0.01 µM for JAK2, 0.01-0.1 µM for JAK3, and ≤0.01 µM for Tyk2, indicating potent activity across these targets. It is utilized in cancer research [1].

JAK-IN-20 is a potent, orally active, broad-based JAK inhibitor, capable of acting on JAK1 (IC50: 7 nM), JAK2 (IC50: 5 nM), and JAK3 (IC50: 14 nM).JAK-IN-20 has excellent pharmacokinetic and anti-inflammatory activity in vivo.

JAK-IN-1 shows improved selectivity for JAK3 over JAK1. JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.

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

JAK-IN-29 (Compound 3) is a potent inhibitor of Janus kinases (JAK) [1].

JAK kinase-IN-1 (Example 1) functions as a potent inhibitor targeting the JAK family, which includes TYK2, JAK1, JAK2, and JAK3, with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively [1].

SYK/JAK-IN-1 is a dual SYK/JAK inhibitor with IC50 values of less than 5 nM for both SYK and JAK2.

JAK-IN-17 is a potent inhibitor of JAK . JAK-IN-17 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases.

JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba/F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].

Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, specifically composed of amino acids 475 to 491.

JAK-IN-21 is a selective and potent JAK inhibitor that inhibits JAK1, JAK2, J2V617F and TYK2 with IC50 values of 1.73, 2.04, 109 and 62.9 nM, respectively.

JAK-IN-30 (compound 31) is a water-soluble inhibitor of Janus kinases (JAKs), demonstrating inhibitory potency with half-maximal inhibitory concentration (IC50) values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2. The compound has been identified as having research potential for the treatment of dry eye disease (DED) [1].

JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations. This compound exhibits proapoptotic properties, inhibits histone deacetylation, and impedes STAT3 phosphorylation, demonstrating notable antiproliferative activity against various hematological malignancies and solid tumors [1].

JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).

JAK-IN-24, a JAK inhibitor, exhibits IC50 values of 0.534 nM and 24 nM in the presence of 4 μM and 1 mM ATP, respectively. Additionally, it effectively inhibits STAT5 phosphorylation induced by PBMC IL-15 with an IC50 of 86.171 nM.

JAK-2/3-IN-2 (Compound 3h) is a potent dual inhibitor of JAK2 and JAK3. It exhibits inhibitory activity with IC50 values of 23.85 nM and 18.9 nM against JAK2 and JAK3, respectively [1].

JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.

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

JAK-IN-3 is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.

JAK1-IN-9 (compound 23a) is a potent, selective inhibitor of JAK1, demonstrating an IC50 of 72 nM. It exhibits over 12-fold selectivity against other JAK family members [1].

JAK-IN-23 is an orally active dual JAK/STAT and NF-κB inhibitor that inhibits J AK1 (IC50: 8.9 nM), J AK2 (IC50: 15 nM), and J AK3 (IC50: 46.2 nM). JAK-IN-23 exhibits strong anti-inflammatory effects and can reduce the release of various pro-inflammatory factors.JAK-IN-23 can be used to study inflammatory bowel disease (IBD).

JAK-2-/3-IN-3 (compound ST4j) can be used in lymph derived diseases and leukemia research. JAK-2-/3-IN-3 inhibits JAK2 autophosphorylation and induces apoptosis in a time- and dose-dependent manner. JAK-2-/3-IN-3 is a potent inhibitor of JAK2/3 with IC50 values of 13.00 and 14.86 nM for JAK2 and JAK3, respectively [1].