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JAK

JAK

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.

JAK related products

Structure Cat No. Product Name CAS No. Product Description
SJ-1008030 V51516 SJ-1008030 2863634-96-0 SJ1008030 (compound 8) is a JAK2 PROTAC that selectively degrades JAK2.
SJ10542 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.
TCJL-37 V15932 TCJL-37 1258294-34-6 TCJL37 is a potent, orally bioactive and selective TYK2 inhibitor (antagonist) with Ki of 1.6 nM.
Tkip 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.
TUL-01101 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.
TX-1123 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.
TYK2 JH2-IN-1-d3 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).
TYK2 ligand 1 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).
Tyk2-IN-14 V86065 Tyk2-IN-14 2308520-97-8
Tyk2-IN-15 V83499 Tyk2-IN-15 3010873-44-3
Tyk2-IN-16 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.
Tyk2-IN-17 V88897 Tyk2-IN-17 3010874-31-1 Tyk2-IN-17 (compound 185) is a potent TYK2 inhibitor.
Tyk2-IN-18 V89063 Tyk2-IN-18 3024860-29-2 Tyk2-IN-18 (compound 86) is a potent tyrosine kinase 2 (Tyk2) inhibitor.
Tyk2-IN-18-d5 V83373 Tyk2-IN-18-d5 3018160-63-6
Tyk2-IN-19 V88896 Tyk2-IN-19 2866415-98-5 Tyk2-IN-19 (compound 1) is an orally active and blood-brain barrier permeable Tyk2 inhibitor.
Tyk2-IN-20 V93215 Tyk2-IN-20 3058568-08-1 Tyk2-IN-20 (Example 289) is a potent Tyk2 inhibitor with IC50 value <5 nM.
TyK2-IN-21-d3 V104918 TyK2-IN-21-d3 2583719-08-6 TyK2-IN-21-d3 (compound 3c) is an oral prodrug of tyrosine kinase 2.
Tyk2-IN-22 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.
Tyrphostin AG213 (AG213) 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).
VVD-118313 V51514 VVD-118313 2875046-27-6 VVD-118313 (compound 5a) is a potent selective JAK1.
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