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Results for "

JAK1/2

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50856
    Ruxolitinib
    Maximum Cited Publications
    117 Publications Verification

    INCB18424

    		 JAK Autophagy Mitophagy Apoptosis Cancer
    Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 [1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
    Ruxolitinib
  • HY-50858
    Ruxolitinib phosphate
    Maximum Cited Publications
    117 Publications Verification

    INCB018424 phosphate

    		 JAK Autophagy Mitophagy Cancer
    Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
    Ruxolitinib phosphate
  • HY-162248
    JAK1/2-IN-1

    		JAK Interleukin Related Inflammation/Immunology Cancer
    JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC50 values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC50s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a) [1].
    <em>JAK1/2</em>-IN-1
  • HY-50859
    Ruxolitinib sulfate

    INCB018424 sulfate

    		 JAK Autophagy Cancer
    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
    Ruxolitinib sulfate
  • HY-125019
    iJak-381

    		JAK STAT Inflammation/Immunology
    iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) [1].
    iJak-381
  • HY-13827
    JAK-IN-1
    1 Publications Verification

    		 JAK Inflammation/Immunology
    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.
    <em>JAK</em>-IN-1
  • HY-143885
    JAK1/TYK2-IN-3

    		JAK Inflammation/Immunology
    JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells .
    <em>JAK</em>1/TYK2-IN-3
  • HY-149283
    JAK/HDAC-IN-2

    		JAK HDAC Apoptosis Cancer
    JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers [1].
    <em>JAK</em>/HDAC-IN-2
  • HY-40354A
    Tofacitinib citrate
    45+ Cited Publications

    Tasocitinib citrate; CP-690550 citrate

    		 JAK Apoptosis Bacterial Fungal Influenza Virus Infection Inflammation/Immunology Cancer
    Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
    Tofacitinib citrate
  • HY-145015
    Tuspetinib

    HM43239

    		 FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells [1] .
    Tuspetinib
  • HY-145015A
    Tuspetinib hydrate

    HM43239 hydrate

    		 FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells [1] .
    Tuspetinib hydrate
  • HY-15999
    Cerdulatinib
    5 Publications Verification

    PRT062070; PRT2070

    		 JAK Syk Cancer
    Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
    Cerdulatinib
  • HY-40354AS
    Tofacitinib-d3 citrate

    Tasocitinib-d3 citrate; CP-690550-d3 citrate

    		 Isotope-Labeled Compounds JAK Apoptosis Bacterial Fungal Influenza Virus Infection Inflammation/Immunology Cancer
    Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
    Tofacitinib-d3 citrate
  • HY-15999A
    Cerdulatinib hydrochloride
    5 Publications Verification

    PRT062070 hydrochloride; PRT2070 hydrochloride

    		 Syk JAK Cancer
    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies [1] .
    Cerdulatinib hydrochloride
  • HY-151262
    JAK-IN-23

    		JAK STING NF-κB STAT Inflammation/Immunology
    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) .
    <em>JAK</em>-IN-23

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