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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V51531 | (2R,5S)-Ritlecitinib | 1792180-79-0 | (2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) is a potent and specific JAK3 conjugate (IC50=144.8 nM). |
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V33937 | (3R,4S)-Tofacitinib | 1092578-46-5 | (3R,4S)-Tofacitinib (Tofacitinib Impurity A) is a less active diastereomer/enantiomer of Tofacitinib (CP 690550;tasocitinib; Xeljanz), which is a JAK3 (Janus-Associated kinase) inhibitor and an FDA approved drug for the treatment of rheumatoid arthritis (RA), psoriatic arthritis, and ulcerative colitis. |
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V33936 | (3S,4R)-Tofacitinib | 1092578-48-7 | (3S,4R)-Tofacitinib (Tofacitinib Impurity B) is a less active isomer/enantiomer of Tofacitinib (CP-690550;tasocitinib; Xeljanz), which is an inhibitor of JAK3 (Janus-Associated kinase, IC50 = 1 nM) and an FDA approved drug for the treatment of rheumatoid arthritis (RA), psoriatic arthritis, and ulcerative colitis. |
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V9140 | (3S,4S)-Tofacitinib | 1092578-47-6 | 3S,4S)-Tofacitinib (Tofacitinib Impurity C) is a less active enantiomer of Tofacitinib (tasocitinib; CP-690550; Xeljanz), which is an inhibitor of JAK3 (Janus-Associated kinase) and an FDA approved drug for the treatment of rheumatoid arthritis (RA), psoriatic arthritis, and ulcerative colitis. |
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V56165 | (Rac)-Ruxolitinib-d9 ((Rac)-INCB18424-d9; Ruxotinib racemate-d9) | 2469553-67-9 | (Rac)-Ruxolitinib D9 ((Rac)-INCB18424 D9) is a deuterium labelled form of (Rac)-Ruxolitinib. |
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V86300 | 25-Deacetylcucurbitacin A | 1135141-77-3 | |
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V69735 | ABBV-712 | 2368945-27-9 | ABBV-712 is a selective tyrosine kinase 2 (TYK2) inhibitor (antagonist) with IC50 of 0.195 μM and plays an important role in autoimmune diseases. |
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V4059 | Abrocitinib (PF04965842) | 1622902-68-4 | Abrocitinib (formerly known as PF04965842; PF-04965842; Cibinqo) is a novel, potent and orally bioavailable JAK1 (Janus Kinase 1)inhibitor with immunomodulatory and antiinflammatory effects. |
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V0322 | AG-490 (Tyrphostin B42; zinc0255794) | 133550-30-8 | AG-490 (also known as Tyrphostin B42; zinc-0255794) is a novel, potent and selective inhibitor of EGFR (epidermal growth factor receptor) with potential antitumor activities. |
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V0318 | AT9283 | 896466-04-9 | AT9283 is a novel, potentand selective inhibitor of multikinase including Aurora A/B,JAK2/3,Abl (T315I)andFlt3 etc. |
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V0334 | AZ 960 | 905586-69-8 | AZ 960 (AZ-960) is a novel, potent, selective and ATP competitive JAK2 (janus kinase) inhibitor with potential antitumor activity. |
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V0316 | AZD1480 | 935666-88-9 | AZD1480 (AZD-1480)is a selective, orally bioavailable andATP-competitive inhibitor of JAK2 (Janus-associated kinase)with potential antitumor activity. |
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V0338 | Baricitinib (LY-3009104, INCB-028050) | 1187594-09-7 | Baricitinib, (also known as LY3009104 or INCB028050; trade name:Olumiant), is apotent,selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 (Janus kinase) or JAK2 with anti-inflammatory activity. |
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V0096 | Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant) | 1187595-84-1 | Baricitinib phosphate, the phosphate salt of Baricitinib which is also known as LY3009104 or INCB028050 or trade name Olumiant, is apotent,selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2. |
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V51513 | BD-750 | 892686-59-8 | BD750 is a potent immunological dye for JAK3/STAT5 that can inhibit IL-2-induced, JAK3/STAT5-dependent T cell proliferation/growth. |
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V0319 | BMS-911543 | 1271022-90-2 | BMS-911543 (BMS911543) is a potent, selective and orally bioavailable inhibitor of JAK2 (Janus-associated kinase) with potential anticancer activity. |
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V51526 | Butyzamide | 1110767-45-7 | activator of Mpl |
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V0333 | CEP-33779 | 1257704-57-6 | CEP33779 is a novel, potent,orally bioactive,highly selective inhibitor of JAK2 (Janus kinase) with potential antitumor and anti-inflammatoryactivity. |
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V2659 | Cerdulatinib | 1198300-79-6 | Cerdulatinib (formerly known as PRT2070 and PRT062070) is an oral bioactive, dual-targeted tyrosine kinase (JAK and Syk) inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk [spleen tyrosine kinase (SYK) and Janus kinase (JAK)], respectively. |
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V0325 | Cerdulatinib HCl (PRT-2070; PRT-062070) | 1369761-01-2 | Cerdulatinib HCl (formerly PRT2070; PRT062070) is a novel, potent, selective orally bioactive, and multi-targeted tyrosine kinase inhibitor ofJAK1/2/3/TYK2 and Syk with potential antitumor activity. |
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