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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V51516 | SJ-1008030 | 2863634-96-0 | SJ1008030 (compound 8) is a JAK2 PROTAC that selectively degrades JAK2. |
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V53150 | SJ10542 | 2789678-92-6 | SJ10542 is a potent and specific JAK2/3-directed phenylglutarimide (PG)-PROTAC with DC50s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. |
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V15932 | TCJL-37 | 1258294-34-6 | TCJL37 is a potent, orally bioactive and selective TYK2 inhibitor (antagonist) with Ki of 1.6 nM. |
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V106289 | Tkip | 716361-65-8 | Tkip is a specific inhibitor of JAK2. It can bind to the JAK2 autophosphorylation site, inhibit JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1, inhibit the antiviral activity of IFN-γ and the expression of MHC class I molecules, and can be used for research related to the IFN-γ signaling pathway. |
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V51510 | TUL-01101 | 2411222-97-2 | TUL01101 is a specific and orally bioactive JAK1 inhibitor (antagonist) with IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3 and TYK2 respectively. |
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V35164 | TX-1123 | 157397-06-3 | TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor targeting Src, eEF2-K, PKA and EGFR-K/PKC. |
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V56092 | TYK2 JH2-IN-1-d3 | 2376999-19-6 | TYK2 JH2-IN-1-d3 is a deuterated, orally bioactive and selective TYK2 inhibitor (compound 4h) targeting the JH2 domain (IC50=0.1 nM). |
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V88973 | TYK2 ligand 1 | 2770471-05-9 | TYK2 ligand 1 is a ligand of TYK2 and can be used to synthesize TYK2 PROTAC degrader (CPD-155). |
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V86065 | Tyk2-IN-14 | 2308520-97-8 | |
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V83499 | Tyk2-IN-15 | 3010873-44-3 | |
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V88969 | Tyk2-IN-16 | 3010874-30-0 | Tyk2-IN-16 is a selective and potent TYK2 inhibitor with IC50 of <10 nM for TYK2-JH2. |
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V88897 | Tyk2-IN-17 | 3010874-31-1 | Tyk2-IN-17 (compound 185) is a potent TYK2 inhibitor. |
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V89063 | Tyk2-IN-18 | 3024860-29-2 | Tyk2-IN-18 (compound 86) is a potent tyrosine kinase 2 (Tyk2) inhibitor. |
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V83373 | Tyk2-IN-18-d5 | 3018160-63-6 | |
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V88896 | Tyk2-IN-19 | 2866415-98-5 | Tyk2-IN-19 (compound 1) is an orally active and blood-brain barrier permeable Tyk2 inhibitor. |
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V93215 | Tyk2-IN-20 | 3058568-08-1 | Tyk2-IN-20 (Example 289) is a potent Tyk2 inhibitor with IC50 value <5 nM. |
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V104918 | TyK2-IN-21-d3 | 2583719-08-6 | TyK2-IN-21-d3 (compound 3c) is an oral prodrug of tyrosine kinase 2. |
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V104314 | Tyk2-IN-22 | 933667-23-3 | Tyk2-IN-22 (Compound A8) is a selective inhibitor of tyrosine kinase 2 (Tyk2), inhibiting Tyk2, JAK1 and JAK3 with IC50 of 9.7, 148.6 and 883.3 nM, respectively. |
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V35163 | Tyrphostin AG213 (AG213) | 122520-86-9 | Tyrphostin AG213 (AG213) is an epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor (IC50=0.85 μM). |
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V51514 | VVD-118313 | 2875046-27-6 | VVD-118313 (compound 5a) is a potent selective JAK1. |