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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
JAK1/TYK2-IN-4 V85952 JAK1/TYK2-IN-4 2734918-33-1
JAK2 JH2 binder-1 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.
JAK2-IN-10 V88892 JAK2-IN-10 3035735-18-0 JAK2-IN-10 (Compound 5) is a potent JAK2 v617f inhibitor with IC50 value of ≤10 nM.
JAK2-IN-11 V104598 JAK2-IN-11 3057053-17-2 JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with an IC50 of ≤10 nM for JH2 BIND WT/V617F.
JAK2-IN-6 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.
JAK2-IN-7 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.
JAK2-IN-9 V56095 JAK2-IN-9 2568842-26-0 JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50= 5 nM).
JAK2/FLT3-IN-1 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.
JAK3-IN-13 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.
JAK3-IN-14 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.
JAK3-IN-15 V97141 JAK3-IN-15 JAK3-IN-15 (Compound 22) is a JAK3 inhibitor that reduces LPS-induced p-JAK3 secretion.
JAK3-IN-16 V105056 JAK3-IN-16 1962125-80-9 JAK3-IN-16 (Compound 6) is a covalent JAK3 inhibitor.
JAK3-IN-6 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.
JANEX-1 hydrochloride V88972 JANEX-1 hydrochloride 188829-39-2 JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor with Ki of 2.3 μM and IC50 of 78 μM.
JNK-1-IN-1 V51539 JNK-1-IN-1 1262406-02-9 JNK-1-IN-1 is a JNK-1 benchmark.
JNK3 inhibitor-1 V51541 JNK3 inhibitor-1 2622877-97-6 JNK3 Inhibitor-1 is a potent and potent JNK3 inhibitor (IC50 = 0.005 μM).
JNK3 inhibitor-4 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.
JNK3 inhibitor-5 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.
JNK3 inhibitor-7 V51540 JNK3 inhibitor-7 JNK3 inhibitor-7 is a potent, orally bioactive JNK3 inhibitor that can cross the BBB (blood-brain barrier).
Lepzacitinib V52920 Lepzacitinib 2321488-47-3 Lepzacitinib is a Janus kinase inhibitor targeting JAK 1/3.
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