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

JAK

Janus kinase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15166B
    (E/Z)-Zotiraciclib citrate
    Inhibitor 99.83%
    (E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.
    (E/Z)-Zotiraciclib citrate
  • HY-174280
    Modzatinib
    Inhibitor
    Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases.
    Modzatinib
  • HY-W722277A
    LCC-12 formate
    Inhibitor 99.9%
    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-N3011
    Iridin
    Inhibitor 99.72%
    Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.
    Iridin
  • HY-173357
    TYD-68
    Degrader 99.54%
    TYD-68 is a highly efficient and selective CRBN-recruited TYK2 PROTAC degrader with a DC50 value of 0.42 nM. TYD-68 significantly inhibits IL-12 and IFN-α-induced STAT4 and STAT1 phosphorylation, thereby blocking TYK2-dependent signaling pathways. TYD-68 can be used in the study of psoriasis. (Pink: Target protein ligand (HY-173359); Black: Linker (HY-W007732B); Blue: E3 ligase ligand (HY-14658); E3 ligase ligand + Linker (HY-173358)).
    TYD-68
  • HY-147330B
    SJ1008030 formic
    Inhibitor 98.91%
    SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia.
    SJ1008030 formic
  • HY-107586
    Demethylasterriquinone B1
    Activator 98.10%
    Demethylasterriquinone B1 (DAQ B1; L-783281) is an orally active insulin receptor (insulin receptor) agonist and AKT activator. By activating AKT, Demethylasterriquinone B1 upregulates the expression and activity of eNOS to increase NO production, while downregulating the expression of the NADPH oxidase subunit p22phox to reduce oxidative stress and improve vascular endothelial dysfunction in hypertensive rats. Demethylasterriquinone B1 combind with an AKT inhibitor targets the insulin signaling pathway to activate two antiviral pathways, RNA interference and JAK/STAT, in mosquitoes, thereby reducing Zika virus infection.
    Demethylasterriquinone B1
  • HY-153050
    JAK-IN-24
    Inhibitor 99.35%
    JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM. JAK-IN-24 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    JAK-IN-24
  • HY-101762
    TyK2-IN-2
    Inhibitor 99.05%
    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
    TyK2-IN-2
  • HY-13895
    WHI-P154
    Inhibitor 98.77%
    WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
    WHI-P154
  • HY-111745
    Tyk2-IN-5
    Inhibitor 99.35%
    Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
    Tyk2-IN-5
  • HY-172581
    Clifutinib
    Inhibitor 99.59%
    Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.
    Clifutinib
  • HY-174905
    Quecitinib
    Inhibitor 99.56%
    Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases.
    Quecitinib
  • HY-131906
    JAK2-IN-7
    Inhibitor 98.31%
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
    JAK2-IN-7
  • HY-145588A
    Povorcitinib phosphate
    Inhibitor 98.82%
    Povorcitinib (INCB54707) phosphate is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib phosphate can be used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1).
    Povorcitinib phosphate
  • HY-13827
    JAK-IN-1
    Inhibitor 98.39%
    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
    JAK-IN-1
  • HY-100754C
    Ritlecitinib tosylate
    Inhibitor 99.65%
    Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).
    Ritlecitinib tosylate
  • HY-W062703S
    (Rac)-Ruxolitinib-d9
    Inhibitor 99.44%
    (Rac)-Ruxolitinib D9 ((Rac)-INCB18424 D9) is the deuterium labeled (Rac)-Ruxolitinib. (Rac)-Ruxolitinib is a JAK2 inhibitor.
    (Rac)-Ruxolitinib-d<sub>9</sub>
  • HY-N2282
    Zingiberen newsaponin
    Inhibitor 99.68%
    Zingiberen Newsaponin (Zingiberensis newsaponin) is an orally active type of steroid saponin compound. Zingiberen Newsaponin exerts anti-hepatocellular carcinoma (HCC) effects by inhibiting autophagy and the AKR1C1/JAK2/STAT3 pathway. Zingiberen Newsaponin activates oxidative stress (upregulates ROS and MDA) and mitochondrial pathways, promoting cancer cell apoptosis. Zingiberen Newsaponin alleviates cerebral ischemia-reperfusion (I/R) injury by decreasing the concentration of pro-inflammatory cytokines and inhibits NF-κB. Zingiberen Newsaponin can enhance the activity of SOD, eliminate free radicals and protect nerve cells. Zingiberen Newsaponin induces platelet aggregation.
    Zingiberen newsaponin
  • HY-N3239
    Mulberrofuran G
    Inhibitor
    Mulberrofuran G is a NOX inhibitor (IC50: 6.9 μM) and tyrosinase inhibitor. Mulberrofuran G exhibits anti-inflammatory, antioxidant, antiviral, antitumor, and neuroprotective effects. Mulberrofuran G can be used in the research of tumors, nervous system diseases, and other conditions.
    Mulberrofuran G
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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