2. Signaling Pathways
  3. Epigenetics
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  4. JAK

JAK

Janus kinase

JAK

Related Products

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Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. Since members of the type I and type II cytokine receptor families possess no catalytic kinase activity, they rely on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associate with a proline-rich region in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. After the receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces a conformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate transcription of selected genes.

JAK Isoform Specific Products:

JAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100538
    DTP3
    		Inhibitor 98.45%
    DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
    DTP3
  • HY-111471A
    JAK-IN-5 hydrochloride
    		Inhibitor 99.52%
    JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
    JAK-IN-5 hydrochloride
  • HY-161683
    Tyk2-IN-19
    		Inhibitor 98.62%
    Tyk2-IN-19 (Compound 1) is an orally active and blood-brain barrier (BBB) permeable Tyk2 inhibitor. Tyk2-IN-19 can be used for study of neurodegenerative diseases.
    Tyk2-IN-19
  • HY-50856S
    Deuruxolitinib
    		Inhibitor 99.18%
    Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata.
    Deuruxolitinib
  • HY-151262
    JAK-IN-23
    		Inhibitor 98.88%
    JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
    JAK-IN-23
  • HY-11067
    WHI-P97
    		Inhibitor 99.16%
    WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.
    WHI-P97
  • HY-18313
    S6K1-IN-1
    		Inhibitor 99.71%
    S6K1-IN-1 is a selective S6K1 inhibitor with an IC50 value of 52 nM. S6K1-IN-1 can be used in the research of obesity and insulin resistance-related diseases.
    S6K1-IN-1
  • HY-N7694
    Isotoosendanin
    		Inhibitor 99.51%
    Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation.
    Isotoosendanin
  • HY-115452
    G5-7
    		Inhibitor 98.45%
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
    G5-7
  • HY-15504A
    RGB-286638 free base
    		Inhibitor 98.09%
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638 free base
  • HY-N0918
    Desmethoxyyangonin
    		Inhibitor 99.00%
    Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation.
    Desmethoxyyangonin
  • HY-12538
    Graveoline
    		Inhibitor 99.93%
    Graveoline (Rutamine) is an orally active alkaloid with various activities such as antifungal, antiparasitic, anti-inflammatory, and antitumor effects. Graveoline can induce tumor cell apoptosis and autophagy through a reactive oxygen species-mediated pathway. Graveoline has an MIC of 500 μg/mL for Candida albicans. Graveoline can be used in the research of various diseases such as tumors and liver injury.
    Graveoline
  • HY-12589
    ZM39923 hydrochloride
    		Inhibitor 99.84%
    ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
    ZM39923 hydrochloride
  • HY-160144S
    Lomedeucitinib
    		Inhibitor 99.75%
    Lomedeucitinib (BMS-986322) is a tyrosine protein kinase (TYK2) inhibitor.
    Lomedeucitinib
  • HY-15163
    Zotiraciclib
    		Inhibitor 99.88%
    Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM, respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma.
    Zotiraciclib
  • HY-109182
    Lorpucitinib
    		Inhibitor 99.95%
    Lorpucitinib (JNJ-64251330) is an orally active pan-JAK inhibitor with good enteric selectivity and safety. Lorpucitinib can inhibit the JAK/STAT pathway and reduce the levels of inflammatory biomarkers in serum. Lorpucitinib can be used in the research of familial adenomatous polyposis and gastrointestinal inflammatory diseases.
    Lorpucitinib
  • HY-109179
    Itacnosertib
    		Inhibitor 99.06%
    Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib exhibits anti-leukemic activity.
    Itacnosertib
  • HY-18009
    (Z)-LFM-A13
    		Inhibitor 99.80%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
    (Z)-LFM-A13
  • HY-W722277A
    LCC-12 formate
    		Inhibitor 99.90%
    LCC-12 (formate) is a copper (II) chelator and a derivative of the biguanide metformin (HY-B0627). LCC-12 (formate) reduces its hydrogen peroxide-dependent oxidation of NADH to NAD+. LCC-12 (formate) reduces IL-1β, IL-2, IL-6, IL-8, and TNF-α levels, as well as JAK2, STAT2, and IL-1 receptor-associated kinase 4 (IRAK4) levels in primary human cytokine-activated monocyte-derived macrophages (MDMs). LCC-12 (formate) reduces the number of CD80+ and CD86+ cytokine-activated MDMs. LCC-12 LCC-12 (formate) improves survival in a mouse model of sepsis induced by LPS or cecal ligation and puncture.
    LCC-12 formate
  • HY-15814
    HG-7-85-01
    		Inhibitor 98.14%
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
    HG-7-85-01
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
JAK Isoform Comparison

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