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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
MMT3-72-M2 V85953 MMT3-72-M2 936091-74-6
Momelotinib (LM1149; CYT387; CYT11387) 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.
Niclosamide olamine (BAY2353 olamine) V34785 Niclosamide olamine (BAY2353 olamine) 1420-04-8 Niclosamide (BAY2353) olamine is an orally bioactive antihelmintic compound utilized in the research of parasitic infections.
Niclosamide-13C6 monohydrate (BAY2353-13C6 monohydrate) 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.
Nifuroxazide-d4 (硝呋齐特 d4) V56221 Nifuroxazide-d4 (nifuroxazide d4) 1188487-83-3 Nifuroxazide-d4 is the deuterium labelled form of Nifuroxazide.
Nimucitinib V51517 Nimucitinib 2740557-24-6 Nimucitinib is a Janus kinase (JAK) inhibitor
NSC-370284 V41092 NSC-370284 116409-29-1 NSC-370284 is a selective inhibitor of 10-11 translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC).
NVP-BSK805 V32016 NVP-BSK805 NVP-BSK805 is a novel, potent and selective ATP-competitive JAK2 inhibitor withIC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
NVP-BSK805 V69736 NVP-BSK805 1092499-93-8 NVP-BSK805 is an ATP-competitive JAK2 inhibitor (antagonist) with IC50s of 0.48 nM, 31.63 nM, 18.68 nM and 10.76 nM for JAK2 JH1 (JAK homolog 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
NVP-BSK805 2HCl (BSK-805) V0336 NVP-BSK805 2HCl (BSK-805) 1942919-79-0 NVP-BSK805 2HCl (BSK805), the dihydrochloride salt of NVP-BSK805, is a novel, potent, selective and ATP-competitive JAK2 (Janus kinase) inhibitor with potential antitumor activity.
NVP-BSK805 trihydrochloride V51507 NVP-BSK805 trihydrochloride 2320258-95-3 NVP-BSK805 triHClide is an ATP-competitive JAK2 ligand with IC50s of 0.48 nM, 31.63 nM, 18.68 nM and 10.76 nM for JAK2 JH1 (JAK homolog 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
Oclacitinib (PF-03394197) V3419 Oclacitinib (PF-03394197) 1208319-26-9 Oclacitinib (formerly also known as PF-03394197) is a novel and potent inhibitor of JAK (Janus kinase) family members with IC50 values ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM.
Oclacitinib maleate (PF-03394197) V2550 Oclacitinib maleate (PF-03394197) 1640292-55-2 Oclacitinib maleate (formerly PF-03394197 maleate) is a novel and potent inhibitor of JAK (Janus kinase) family members with IC50 values ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM.
Pacritinib (SB1518) V0331 Pacritinib (SB1518) 937272-79-2 Pacritinib (formerly also known as SB-1518;SB1518; trade name Vonjo)is a novel, potent, selective, andorally bioavailable inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with potential antitumor activity.
Pacritinib citrate (SB1518 citrate) V86138 Pacritinib citrate (SB1518 citrate) 1228923-42-9
Peficitinib (ASP-015K, JNJ-54781532) V0321 Peficitinib (ASP-015K, JNJ-54781532) 944118-01-8 Peficitinib (formerly ASP015K and JNJ54781532)is a novel, potent and orally bioavailable inhibitor ofJanus kinase-JAK with potential anti-inflammatory activities.
PF-06700841 tosylate V3802 PF-06700841 tosylate 2140301-96-6 Brepocitinib (PF-06700841) tosylate, the tosylate salt ofBrepocitinib,isa conformationally constrained piperazinyl-pyrimidine-based, Type 1 ATP site inhibitor of TYK2 and JAK1 kinases with IC50 values of 23 nM and 17 nM respectively.
Povorcitinib  (INCB-54707) V51190 Povorcitinib (INCB-54707) 1637677-22-5 Povorcitinib is a potent and specific JAK1 inhibitor.
Protosappanin A V13300 Protosappanin A 102036-28-2 Protosappanin A is a novel and potent immunosuppressive agentisolated fromCaesalpinia sappanL.
Pumecitinib V51520 Pumecitinib 2401057-12-1 Pumecitinib is a JAK inhibitor (antagonist) with anti~inflammatory activity.
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