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Dyrk1A-IN-1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-146221
    Dyrk1A-IN-5

    		DYRK Neurological Disease
    Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research .
    <em>Dyrk</em>1A-IN-5
  • HY-132308
    DYRK1-IN-1
    1 Publications Verification

    		 DYRK Neurological Disease
    DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .
    <em>DYRK</em>1-IN-1
  • HY-147066
    Dyrk1A-IN-4

    		DYRK Cancer
    Dyrk1A-IN-4 (compound 48) is a potent and orally active DYRK1A and DYRK2 inhibitor with IC50s of 2 nM and 6 nM, respectively. Dyrk1A-IN-4 has anticancer effects .
    <em>Dyrk</em>1A-IN-4
  • HY-139830
    Dyrk1A-IN-1

    		DYRK Neurological Disease
    Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
    <em>Dyrk1A-IN-1</em>
  • HY-162107
    Dyrk1A-IN-6

    		DYRK Neurological Disease
    Dyrk1A-IN-6 (compound 7cc) is an EGCG-like non-competitive inhibitor of DYRK1A. Dyrk1A-IN-6 can be used to alleviate cognitive defects in Down syndrome models .
    <em>Dyrk</em>1A-IN-6
  • HY-147760
    Dyrk1A-IN-2

    		DYRK Metabolic Disease
    Dyrk1A-IN-2 (Compound 63) is a DYRK1A inhibitor with an EC50 of 37 nM. Dyrk1A-IN-2 exhibits highly potent human β-cell replication-promoting activity and low cytotoxicity .
    <em>Dyrk</em>1A-IN-2
  • HY-146337
    Dyrk1A/B-IN-1

    		DYRK Cancer
    Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable DYRK1A and DYRK1B inhibitor with Kis of 67.8 nM and 237.9 nM, and IC50s of 1.1 μM and 0.8 μM, respectively. Dyrk1A/B-IN-1 is not toxic to human cells. Dyrk1A/B-IN-1 can be used for researching DYRK1A and DYRK1B cellular functions and their role in pathologies .
    <em>Dyrk</em>1A/B-IN-1
  • HY-144695
    Dyrk1A/α-synuclein-IN-1

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
    <em>Dyrk</em>1A/α-synuclein-IN-1
  • HY-144696
    Dyrk1A/α-synuclein-IN-2

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
    <em>Dyrk</em>1A/α-synuclein-IN-2
  • HY-157995
    Dyrk1A-IN-7

    		DYRK Metabolic Disease Inflammation/Immunology Cancer
    Dyrk1a-in-7 (Compound 29) is a selective DYRK1A kinase inhibitor, and has good kinase selectivity for CLK1 kinase. The IC50 value of DYRK1A is 28 nM. For CLK2, Kd is 17.5 nM. Dyrk1a-in-7 can be used in the research of cancer, type Ⅱ diabetes and neurological diseases .
    <em>Dyrk</em>1A-IN-7
  • HY-147060
    Dyrk1A-IN-3

    		DYRK Neurological Disease
    Dyrk1A-IN-3 (Compound 8b), a highly selective  dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
    <em>Dyrk</em>1A-IN-3
  • HY-111379
    EHT 5372

    		DYRK CDK GSK-3 Neurological Disease Metabolic Disease Cancer
    EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .
    EHT 5372
  • HY-149262
    CLK1-IN-3

    		CDK DYRK Autophagy Cancer
    CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research .
    CLK1-IN-3
  • HY-112296
    T025
    2 Publications Verification

    		 CDK Apoptosis DYRK Cancer
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
    T025

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