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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V51503 | JAK-IN-24 | 2042629-43-4 | JAK-IN-24 is a JAK activator with IC50 of 0.534 and 24 nM in the presence of 4 μM or 1 mM ATP, respectively. |
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V51488 | JAK-IN-25 | 2127110-22-7 | JAK-IN-25 (compound 19) is a potent JAK transcript with IC50s of 6 nM, 21 nM, 8 nM, and 1051 nM for TYK2, JAK1, JAK2, and JAK3, respectively. |
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V56091 | JAK-IN-26 | 2417134-93-9 | JAK-IN-26 (compound 2) is an orally bioactive JAK inhibitor (antagonist) with good pharmacokinetic characteristics. |
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V56099 | JAK-IN-27 | 2673176-36-6 | JAK-IN-27 (compound 1) is an orally bioavailable inhibitor of JAK family kinases with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), and 629.6 nM (JAK3). |
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V56096 | JAK-IN-28 | 2445500-22-9 | JAK-IN-28 (Compound 111) is a JAK inhibitor. |
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V56093 | JAK-IN-30 | 2891469-99-9 | JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor (antagonist) with IC50s of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. |
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V56094 | JAK-IN-31 | 2597016-88-9 | JAK-IN-31 (Example 75) is a JAK inhibitor (antagonist) with IC50 ranges of ≤0.01µM, ≤0.01µM, 0.01-0.1 µM and ≤0.01µM for JAK1, JAK2, JAK3 and Tyk2 respectively. |
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V69737 | JAK-IN-34 | 2068766-90-3 | JAK-IN-34 is effective against JAKs, with IC50s of 0.40, 0.83, 2.10, and 1.95 nM targeting JAK1, JAK2, JAK3, and TYK2 respectively. |
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V53260 | JAK-IN-5 hydrochloride | 2751323-21-2 | JAK-IN-5 HCl is an inhibitor (blocker/antagonist) of JAK, disclosed in patent US20170121327A1, example compound 283. |
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V56100 | JAK-STAT-IN-1 | 1236666-76-4 | JAK-STAT-IN-1 (compound 1) is a selective JAK-STAT inhibitor. |
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V51485 | JAK/HDAC-IN-3 | JAK/HDAC-IN-3 (13a) is a dual (bifunctional) inhibitor of JAK and HDAC, with IC50s of 25.36 nM, 0.2 μM, and 0.43 μM for JAK2, HDAC, and HDAC1, respectively. | |
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V51500 | JAK1-IN-10 | 2416858-88-1 | JAK1-IN-10 (compound 9) is a cyano-substituted cyclic hydrazine analogue and a potent and selective inhibitor of JAK1. |
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V56098 | JAK1-IN-11 | 2427608-43-1 | JAK1-IN-11 (compound 11) is a potent JAK inhibitor (antagonist) with IC50 of 0.02 nM (JAK1) and 0.44 nM (JAK2). |
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V51489 | JAK1-IN-12 | JAK1-IN-12 is a selective JAK1 inhibitor (antagonist) with IC50 of 0.0246 μM for JAK1 and IC50s value of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2 respectively. | |
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V12079 | JAK1-IN-4 | 2091134-35-7 | JAK1-IN-4 is a novel and potent JAK1-selective kinase inhibitor with immunomodulatory effects. |
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V51502 | JAK1-IN-8 | 1973485-18-5 | JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, obtained from patent WO2016119700A1. |
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V51493 | JAK1-IN-9 | 2875041-96-4 | JAK1-IN-9 (compound 23a) is a potent and specific JAK1 with IC50 of 72 nM. |
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V51504 | JAK1/TYK2-IN-1 | 1883300-48-8 | JAK1/TYK2-IN-1 is a dual (bifunctional) inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM). |
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V51505 | JAK2 JH2 binder-1 | 2923309-41-3 | JAK2 JH2 bond-1 (compound 11) is a potent and specific JAK2 JH2 binder with a Kd of 37.1 nM. |
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V51490 | JAK2-IN-6 | 353512-04-6 | JAK2-IN-6 is a polysubstituted thiazole sulfonic acid that is effective and selective for JAK2 coupling with IC50 of 22.86 μg/mL. |
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