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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V83499 | Tyk2-IN-15 | 3010873-44-3 | |
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V83373 | Tyk2-IN-18-d5 | 3018160-63-6 | |
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V35163 | Tyrphostin AG213 (AG213) | 122520-86-9 | Tyrphostin AG213 (AG213) is an epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor (IC50=0.85 μM). |
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V4510 | Upadacitinib tartrate | 1607431-21-9 | Upadacitinib tartrate (formerly ABT494; ABT-494; rinvoq), the tartrate salt ofUpadacitinib, is a novel, potent and selective Janus kinase (JAK) 1 inhibitor approved in 2019 for the treatment of rheumatoid arthritis. |
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V51514 | VVD-118313 | 2875046-27-6 | VVD-118313 (compound 5a) is a potent selective JAK1. |
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V3972 | WHI-P97 | 211555-05-4 | WHI-P97 is a novel, rationally designed, and potent inhibitor of Janus kinase (JAK)-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays. |
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V0330 | XL019 | 945755-56-6 | XL019 is a novel,potent and selective and orally bioavailable inhibitor of Janus kinase-JAK2 with potential antitumor activity. |
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V50938 | Zasocitinib (NDI-034858) | 2272904-53-5 | Zasocitinib (NDI-034858) is a Tyk2 inhibitor that targets the JH2 domain of Tyk2 with a binding constant Kd <200 pM. |
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V0329 | ZM 39923 HCl | 1021868-92-7 | ZM 39923 HCl, the hydrochloride salt of ZM-39923,is a novel and potent inhibitor of Janus kinase-JAK1/3 with potential anti-inflammatory activity. |
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V51523 | ZT-55 | 2138488-38-5 | ZT55 is an effective and selective JAK2 mold with IC50 of 0.031 μM. |
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