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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V0332 | Curcumol | 4871-97-0 | Curcumol is a selective, potent, naturally occuring and pure monomer isolated from Rhizoma Curcumaeis with potential antitumor activities. |
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V0320 | Decernotinib (VX-509; VRT-831509; adelatinib) | 944842-54-0 | Decernotinib (VX509; VRT831509; adelatinib) is a novel, potent, selective, and orally bioavailable inhibitor of JAK3 (Janus associated kinase) with potential anti-inflammatory activities. |
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V19534 | Delgocitinib (LEO124249; JTE052) | 1263774-59-9 | Delgocitinib (formerly LEO-124249; JTE052; LEO124249; JTE-052;Corectim) is a potent and selective JAK inhibitor with anti-inflammatory activities and has been approved in 2020 for use in Japan for the treatment of autoimmune disorders and hypersensitivity, including inflammatory skin conditions (e. |
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V54452 | Disitamab (RC48-0) | 2185868-98-6 | Disitamab (RC48-0) is a humanized monoclonal antibody (mAb) targeting HER2. |
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V34834 | Disitamab vedotin (RC48) | 2136633-23-1 | Disitamab vedotin (RC48) is an antibody-active molecule conjugate (ADC) containing a monoclonal antibody (mAb) against human epidermal growth factor receptor 2 (HER2) conjugated to a cytotoxic agent via a degradable linker MMAE. |
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V35047 | Erlotinib-13C6 (CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6) | 1211107-68-4 | Erlotinib-13C6 is a 13C (carbon 13)-labeled Erlotinib. |
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V56522 | Erlotinib-13C6 hydrochloride (CP-358774-13C6 hydrochloride; NSC 718781-13C6 hydrochloride; OSI-774-13C6 hydrochloride) | 1210610-07-3 | Erlotinib-13C6 ( HCl) is a 13C (carbon 13)-labeled Erlotinib HCl. |
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V0317 | Fedratinib (SAR302503) | 936091-26-8 | Fedratinib (formerly SAR302503 or TG101348; brand name Inrebic) is a novel, potent, selective, orally bioavailable, small-molecule and ATP-competitive inhibitor of janus kinase 2 (JAK2) with an IC50 of 3 nM. |
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V16212 | Fedratinib (TG101348) dihydrochloride hydrate | 1374744-69-0 | Fedratinib dihydrochloride hydrate(SAR302503 or TG101348) is a novel, potent, selective, orally bioavailable, small-molecule and ATP-competitive inhibitor of janus kinase 2 (JAK2) with the inhibition constant IC50 of 3 nM. |
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V0326 | Filgotinib (GLPG-0634) | 1206161-97-8 | Filgotinib (also known as GLPG0634; GLPG-0634;Jyseleca) is a novel, potent and selective JAK1 (Janus kinase) inhibitor with potential anti-inflammatory activity. |
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V51509 | Filgotinib-d4 | 2041095-50-3 | Filgotinib-d4 is the deuterated form of Filgotinib. |
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V0324 | FLLL32 | 1226895-15-3 | FLLL32, a synthetic curcumin analog, is a novel and potent Janus kinases-JAK2/STAT3 inhibitor with potential antitumor activity. |
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V4533 | FM-479 | 2226521-64-6 | FM 479 (FM479) is a negative control for FM-381 withno activity on JAK3 or other kinases. |
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V2327 | G5-7 | 939681-36-4 | G5-7 is an orally bioactive allosteric inhibitor of JAK2 that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2. |
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V0341 | Gandotinib (LY-2784544) | 1229236-86-5 | Gandotinib (formerly also known as LY2784544) is a novel, potent and selective JAK2 (Janus kinase) inhibitorwith potential antitumor activity. |
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V51511 | GDC-046 | 1258292-64-6 | GDC-046 is a potent, active and selective TYK2 antagonist (inhibitor) with Ki of 4.8, 0.7, 0.7 and 0.4 nM for TYK2, JAK1, JAK2 and JAK3 respectively. |
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V51522 | GDC-4379 | 2252277-73-7 | GDC-4379 is a JAK1 inhibitor for asthma research. |
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V56491 | Gefitinib-d3 (gefitinib d3) | 1173976-40-3 | Gefitinib-d3 is the deuterated form of Gefitinib. |
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V56475 | Gefitinib-d6 (ZD1839-d6) | 1228664-49-0 | Gefitinib-d6 is the deuterated form of Gefitinib. |
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V0328 | GLPG0634 analogue | 1206101-20-3 | GLPG0634 analogue, an analog ofFilgotinib (GLPG0634),is a novel, potent andselective Janus kinase-JAK1 inhibitor with potential anti-inflammatory activity. |
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