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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V88891 | (1R)-AZD-1480 | 935666-99-2 | (1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP-competitive JAK1 and JAK2 inhibitor. |
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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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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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V88970 | AC-430 hydrobromide | 1359828-49-1 | AC-430 hydrobromide is a potent JAK2 inhibitor. |
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V88899 | AMPK-IN-5 | AMPK-IN-5 (compound 7m) is an osthole derivative that blocks MAPK signaling by inhibiting the phosphorylation of JNK and p38, thereby suppressing the release of inflammatory cytokines. | |
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V87061 | anti-TNBC agent-7 | anti-TNBC agent-7 (Compound 13c) has anti-cancer activity and can be used as a molecular probe to recognize and regulate the signaling of the USP21/JAK2/STAT3 axis, with nanomolar levels against MDA-MB-231 and HCC-1806 cancer cells. | |
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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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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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V91786 | BVB808 | 1414587-22-6 | BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. |
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V93752 | Cenacitinib | 2641636-52-2 | Cinatinib is a potent Janus kinase inhibitor. |
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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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V3373 | CHZ868 | 1895895-38-1 | CHZ868 is a novel, potent and selective type IIJAK2inhibitor with anIC50of 0.17 μM in EPOR JAK2 WT Ba/F3 cell. |
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