JAK

JAK

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway.Members of the type I and type II cytokine receptor families depend on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways because they lack catalytic kinase activity. The receptors have two intracellular signal-transducing domains because they are paired polypeptides. Each intracellular domain contains a proline-rich region called a box1/box2 region that is close to the cell membrane and where JAKs bind. The two JAKs are brought close enough to phosphorylate one another after the receptor undergoes a conformational change following association with the corresponding cytokine or ligand. By further phosphorylating and activating STAT transcription factors, JAK autophosphorylation causes a conformational change within itself, enabling it to transduce the intracellular signal. When STATs are activated, they separate from their receptor and coalesce into dimers before moving into the cell nucleus, where they control the transcription of particular genes.

JAK related products

Structure Cat No. Product Name CAS No. Product Description
V77246 APTSTAT3-9R
V4261 AT-9283 HCl 896466-61-8 AT9283 is a novel, potent multikinase inhibitor with potential antineoplastic activity and has the potential for the treatment of multiple myeloma.
V4262 AT-9283 L-lactate 896466-76-5 AT-9283 L-lactate is a novel, potent multikinase inhibitor with potential antineoplastic activity and has the potential for the treatment of multiple myeloma.
V4455 Brepocitinib (PF-06700841) 1883299-62-4 Brepocitinib (PF06700841; PF-06700841) is a potent, selective, and conformationally constrained piperazinyl-pyrimidine Type 1 ATP site inhibitor of TYK2 and JAK1 kinases with anti-inflammatory effects.
V78833 CMD178
V77144 CMD178 TFA
V4971 Cucurbitacin E 18444-66-1 Cucurbitacin E, a naturally occurring triterpene analog isolated from the climbing stem ofCucumic melo L witha potential therapeutic agent for metabolic diseases, significantly suppresses the activity of the cyclin B1/CDC2 complex.
V4752 Deucravacitinib (BMS-986165) 1609392-27-9 Deucravacitinib (formerly BMS986165; BMS-986165;Tyk2-IN-4; Sotyktu) is a first-in-class, highly potent, orally bioavailable, selective and allosteric inhibitor of TYK2 (tyrosine kinase 2, a JAK family member/enzyme) inPhase 3 clinical studies across multiple immune-mediated diseases such as psoriatic arthritis, lupus and inflammatory bowel disease.
V3114 FM-381 2226521-65-7 FM-381 (FM381) is a potent, specific, covalent reversible inhibitor ofJAK3 with anti-inflammatory activity.
V2144 FM-381 HCl 2226521-65-7 FM-381 HCl is a Chemical Probe For JAK3 and JAK3 specific reversible covalent inhibitor.
V80085 JAK-IN-29
V79111 JAK-IN-33
V3971 JANEX-1 202475-60-3 JANEX-1 (aslo known as WHI-P131) is a novel, potent and selective inhibitor of the Janus kinase 3 (JAK3) that selectively inhibits JAK3 with an IC50 of 78 µM and does not inhibit JAK1 and JAK2.
V80712 MC0704
V4974 NSC-42834 195371-52-9 NSC 42834 (also known as JAK2 Inhibitor V) is a novel, potent and specific inhibitor of JAK2 which inhibits JAK2-V617F and JAK2-WT autophosphorylation in a dose-dependent manner with IC50 values between 10 and 30 µM.
V81001 OK2
V76674 OSM-SMI-10B
V3111 Ritlecitinib (PF-06651600) 1792180-81-4 Ritlecitinib (PF-06651600) is a novel, potent, selective and irreversible/covalent JAK3inhibitor with the potential to treat autoimmune diseases such asarthritis and Alopecia areata.
V31670 Ropsacitinib (PF-06826647; Tyk2-IN-8) 2127109-84-4 Ropsacitinib (PF-06826647; Tyk2-IN-8; PF06826647) is a novel, selective and orally bioavailable TYK2 (tyrosine kinase) inhibitor with potential anti-inflammatory activity.
V76478 STAT3-IN-15
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