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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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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V102608 | (R)-9b | 1655527-68-6 | (R)-9b is a potent ACK1 tyrosine kinase inhibitor (IC50=56 nM) with anticancer activity. |
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V103326 | (R)-α7 nAchR-JAK2-STAT3 agonist 1 | (R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1. | |
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V122044 | (Rac)-TUL01101 | 2411222-71-2 | (Rac)-TUL01101 is a selective JAK kinase inhibitor. |
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V122186 | (S)-Lomedeucitinib | 2328068-38-6 | (S)-Lomedeucitinib is the S-enantiomer of lomedeucitinib. |
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V4262 | AT-9283 L-lactate | 896466-76-5 | AT-9283 L-lactate is a novel, potent multikinase inhibitor with potential antineoplastic activity and has the potential for the treatment of multiple myeloma. |
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V86300 | 25-Deacetylcucurbitacin A | 1135141-77-3 | |
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V127204 | 5TTU | 5TTU is a covalent JAK3 inhibitor. | |
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V115239 | AC-430 | 1241914-87-3 | AC-430 is a JAK2 inhibitor. |
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V77246 | APTSTAT3-9R | APTSTAT3-9R is a specific STAT3-binding peptide that can inhibit STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. | |
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V4261 | AT-9283 HCl | 896466-61-8 | AT9283 is a novel, potent multikinase inhibitor with potential antineoplastic activity and has the potential for the treatment of multiple myeloma. |
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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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V102487 | BPC 157 acetate | 1628202-19-6 | BPC 157 Acetate is the acetate salt form of BPC 157. |
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V3802 | Brepocitinib (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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V51526 | Butyzamide | 1110767-45-7 | activator of Mpl |