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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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. | |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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V51190 | Povorcitinib (INCB-54707) | 1637677-22-5 | Povorcitinib is a potent and specific JAK1 inhibitor. |
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V13300 | Protosappanin A | 102036-28-2 | Protosappanin A is a novel and potent immunosuppressive agentisolated fromCaesalpinia sappanL. |
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V51520 | Pumecitinib | 2401057-12-1 | Pumecitinib is a JAK inhibitor (antagonist) with anti~inflammatory activity. |
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V2962 | Pyridone 6 | 457081-03-7 | Pyridone 6 (also known as P6, CMP 6 or JAK Inhibitor I) is a pan-JAK (Janus-activated kinase) inhibitor with potential anti-AD and anticancer activity. |
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V69738 | QL-1200186 | 2848664-42-4 | QL-1200186 is an orally bioactive and selective TYK2 inhibitor. |
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V51527 | Rovadicitinib | 1948242-59-8 | Rovadicitinib is a JAK inhibitor (antagonist) with IC50 <20 nM. |
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V51525 | Rovadicitinib hydrochloride | 1948242-60-1 | Rovadicitinib HCl is a JAK inhibitor (antagonist) with IC50 <20 nM. |
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V38108 | RSV A405 | 140405-36-3 | RSVA405 is a potent and orally bioactive AMPK activator with EC50 of 1 μM. |
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V0314 | Ruxolitinib (INCB-018424; INC-424) | 941678-49-5 | Ruxolitinib (formerly INC424, INCB18424, INCB018424; trade name Jakafi and Jakavi) is the first-in class, potent, selective, and orally bioavailabe JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3. |
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V0076 | Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi) | 1092939-17-7 | Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which isalso known as INC424, INCB18424 or INCB018424, is a first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3. |
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V0077 | Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi) | 1092939-16-6 | Ruxolitinib sulfate, the sulfate salt of ruxolitinib which isalso known as Jakafi, Jakavi, INC-424, INCB-18424 or INCB-018424, is the first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3. |
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