jak inhibitor

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.

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.

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

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.

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.

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.

JAK3covalent inhibitor-2 (compound J1b) is a selective JAK3 inhibitor with oral efficacy, boasting an IC50 value of 7.2 nM. It is characterized by low toxicity, anti-inflammatory properties, and excellent bioavailability.

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.

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Deucravacitinib is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

Nimbolide, a triterpenoid derived from neem leaves and flowers, is a natural product and a CDK4/CDK6/NF-κB inhibitor that inhibits multiple signaling pathways including Wnt and PI3K-Akt, possesses antitumor activity, and can induce tumor cell apoptosis.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1/2 inhibitor with IC50 of 3.3 nM/2.8 nM. Its selectivity for JAK1/2 is more than 130 times that of JAK3.

Atinvicitinib, a selective Janus kinase (JAK) inhibitor, demonstrates high specificity for Janus kinase 1 (JAK1), consequently inhibiting downstream cytokine signaling pathways that rely on JAK1 enzymatic activity. Atinvicitinib modulates a wide range of cytokines that are implicated in itch responses, allergic reactions, and inflammatory conditions, making it a significant research tool for studying cytokine-mediated immune processes as well as therapeutic modulation of allergic and inflammatory diseases.

Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

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.

Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.

Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

JAK-IN-5 is a JAK inhibitor.

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

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

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