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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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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V85952 | JAK1/TYK2-IN-4 | 2734918-33-1 | |
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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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V51491 | JAK2-IN-7 | 2593402-36-7 | JAK2-IN-7 is a JAK2 selectivity with IC50s of 3, 11.7 and 41 nM for cellular JAK2, SET-2 and Ba/F3V617F. |
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V56095 | JAK2-IN-9 | 2568842-26-0 | JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50= 5 nM). |
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V51499 | JAK2/FLT3-IN-1 | 2387765-27-5 | JAK2/FLT3-IN-1 is an orally bioactive dual JAK2/FLT3 conjugate with IC50s of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. |
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V51551 | JAK3-IN-13 | 2803329-86-2 | JAK3-IN-13 is a specific and orally bioactive JAK3 inhibitor (antagonist) with IC50s of 4728, 2039, 8 and 365 nM for NK1, JNK2, JNK3 and Tyk2 respectively. |
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V53315 | JAK3-IN-14 | 454234-24-3 | JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor (antagonist) with IC50s of 38 nM and 600 nM for JAK3 and JAK2, respectively. |
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V4056 | JAK3-IN-6 | 1443235-95-7 | JAK3-IN-6 is a novel potent, selective, and irreversible inhibitor of Janus Associated Kinase 3 (JAK3) with anti-inflammatory effects. |
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V51539 | JNK-1-IN-1 | 1262406-02-9 | JNK-1-IN-1 is a JNK-1 benchmark. |
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V51541 | JNK3 inhibitor-1 | 2622877-97-6 | JNK3 Inhibitor-1 is a potent and potent JNK3 inhibitor (IC50 = 0.005 μM). |
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V51542 | JNK3 inhibitor-4 | 2409109-65-3 | JNK3 Inhibitor-4 is a potent JNK3 EGFR (IC50=1.0 nM) based on 2-aryl-1-alfalfa-1H-imidazol-5-yl ethyl acetone. |
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V51543 | JNK3 inhibitor-5 | 2911640-63-4 | JNK3 inhibitor-5 (compound 22b) is a potent and rapid JNK3 analogue with IC50 of 0.379 nM. |
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V51540 | JNK3 inhibitor-7 | JNK3 inhibitor-7 is a potent, orally bioactive JNK3 inhibitor that can cross the BBB (blood-brain barrier). | |
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V52920 | Lepzacitinib | 2321488-47-3 | Lepzacitinib is a Janus kinase inhibitor targeting JAK 1/3. |
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V55046 | LRRK2-IN-8 | 2770269-44-6 | LRRK2-IN-8 is an LRRK2 inhibitor. |
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V55047 | LRRK2/NUAK1/TYK2-IN-1 | 2629192-96-5 | LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory effect against LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1 with IC50 less than 10 nM. |
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V85823 | MMT3-72 | 2996158-39-3 |
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