JAK

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.

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

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

JAK-IN-5 is a JAK inhibitor.

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

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

JAK-IN-28 (Compound 111) is a Janus kinase (JAK) inhibitor with potential applicability in cancer and inflammatory disease research [1].

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

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

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

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-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 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].

JAK-IN-30 (compound 31) is a water-soluble Janus kinase (JAK) inhibitor with IC50 values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2, identified for its research potential in treating dry eye disease (DED) [1].

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

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/ 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/ 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.

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].

JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.

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.

JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).

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

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.

JAK1-IN-8, a specific inhibitor of Janus kinase 1 (JAK1, IC50<500 nM).

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.

Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM. It effectively inhibits the phosphorylation of JAK2, STAT3, and STAT5, possesses metabolic stabilities, and induces apoptosis. This compound is utilized in the study of myeloproliferative neoplasms (MPNs) [1].

JAK1-IN-11 (compound 11) is a potent Janus kinase inhibitor with nanomolar IC50 values of 0.02 nM for JAK1 and 0.44 nM for JAK2, demonstrating high selectivity for JAK1 over JAK2 [1].

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective inhibitor of JAK1 [1].

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study

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.

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1 2 inhibitor to enter the clinic with IC50 of 3.3 nM 2.8 nM, >130-fold selectivity for JAK1 2 versus JAK3.

Ruxolitinib (INCB018424) is a JAK1 2 inhibitor (IC50=3.3 2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

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).

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.

Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.

WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.

JI069 (WAY-354189) is a potent STAT3 inhibitor that inhibits gp130 signaling by inducing dissociation between gp130 and JAK1.

SJ1008030 (compound 8) formic is a selective JAK2 degrader from the PROTAC class, exhibiting efficacy in inhibiting MHH-CALL-4 leukemia cell growth with an IC50 of 5.4 nM, and is potentially applicable for leukemia research [1].

SJ1008030 (compound 8), a JAK2 PROTAC, selectively degrades JAK2. It demonstrates potent activity against MHH–CALL-4 cells, with an EC50 of 5.4 nM and an IC50 of 32.09 nM. This compound holds potential for leukemia research [1].