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
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.
V56095 JAK2-IN-9 2568842-26-0 JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50= 5 nM).
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.
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.
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.
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.
V51539 JNK-1-IN-1 1262406-02-9 JNK-1-IN-1 is a JNK-1 benchmark.
V51541 JNK3 inhibitor-1 2622877-97-6 JNK3 Inhibitor-1 is a potent and potent JNK3 inhibitor (IC50 = 0.005 μM).
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.
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.
V51540 JNK3 inhibitor-7 JNK3 inhibitor-7 is a potent, orally bioactive JNK3 inhibitor that can cross the BBB (blood-brain barrier).
V52920 Lepzacitinib 2321488-47-3 Lepzacitinib is a Janus kinase inhibitor targeting JAK 1/3.
V55046 LRRK2-IN-8 2770269-44-6 LRRK2-IN-8 is an LRRK2 inhibitor.
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.
V0323 Momelotinib (LM1149; CYT387; CYT11387) 1056634-68-4 Momelotinib (formerly CYT-387; CYT-11387; LM-1149), an aminopyrimidine analog, is a novel, potent and ATP-competitive inhibitor of Janus kinases (JAK1/2) with potential antitumor and anti-inflammatory activity.
V34785 Niclosamide olamine (BAY2353 olamine) 1420-04-8 Niclosamide (BAY2353) olamine is an orally bioactive antihelmintic compound utilized in the research of parasitic infections.
V56215 Niclosamide-13C6 monohydrate (BAY2353-13C6 monohydrate) 1325559-12-3 Niclosamide-13C6 (monohydrate) is an orally bioactive antihelmintic compound utilized in the research of parasitic infections.
V56221 Nifuroxazide-d4 (nifuroxazide d4) 1188487-83-3 Nifuroxazide-d4 is the deuterium labelled form of Nifuroxazide.
V51517 Nimucitinib 2740557-24-6 Nimucitinib is a Janus kinase (JAK) inhibitor
V41092 NSC-370284 116409-29-1 NSC-370284 is a selective inhibitor of 10-11 translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC).
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