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DYRK1A inhibitor

" in MedChemExpress (MCE) Product Catalog:

57

Inhibitors & Agonists

3

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    Dyrk1A-IN-3
  • HY-146221
    Dyrk1A-IN-5
    1 Publications Verification

    		 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 .
    Dyrk1A-IN-5
  • 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 .
    Dyrk1A-IN-4
  • HY-159496
    Dyrk1A-IN-10

    		DYRK Metabolic Disease
    Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor with antidiabetic activity. Dyrk1A-IN-10 can promote pancreatic β-cell proliferation, increase insulin secretion, and lower blood sugar .
    Dyrk1A-IN-10
  • HY-158212
    Dyrk1A-IN-8

    		DYRK Neurological Disease
    Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A , with the IC50 of 209 nM. Dyrk1A-IN-8 plays an important role in neurodegenerative diseases .
    Dyrk1A-IN-8
  • HY-122989
    Aristolactam BIII

    		DYRK Inflammation/Immunology
    Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models .
    Aristolactam BIII
  • 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 .
    Dyrk1A-IN-6
  • 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 .
    Dyrk1A-IN-7
  • 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 .
    Dyrk1A-IN-2
  • 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.
    Dyrk1A-IN-1
  • HY-170940
    Dyrk1A-IN-12

    		DYRK Enterovirus Infection
    Dyrk1A-IN-12 (compound S43) is a Dyrk (Dual specificity tyrosine phosphorylation regulated kinase 1A inhibitor. Dyrk1A-IN-12 inhibits Dyrk1A with a IC50 of 95 nM. Dyrk1A-IN-12 shows anti-EV-A71 activity with an EC50 of 4.4 μM, CC50 of 12.8 μM and SI of 2.9. Dyrk1A-IN-12 shows potent inhibition against herpes simplex virus (HSV) .
    Dyrk1A-IN-12
  • HY-168265
    Dyrk1A-IN-11

    		DYRK Neurological Disease Cancer
    Dyrk1A-IN-11 (compound 166) is a potent dual-specificity tyrosine phosphorylation- regulated 1A (DYRK1A) inhibitor with an EC50 value of 0.0021 µM. Dyrk1A-IN-11 inhibits the Phospho-Tau (Thr212) with an EC50 value of 0.0361 µM .
    Dyrk1A-IN-11
  • 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 .
    Dyrk1A/B-IN-1
  • HY-132308
    DYRK1-IN-1
    2 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 .
    DYRK1-IN-1
  • HY-W067583
    Norharmine

    		Monoamine Oxidase DYRK Others
    Norharmine is a Harmine analogue and an alkaloid. Norharmine is the inhibitors of MAO-A and DYRK1A. Norharmine has weak inhibitory activity against MAO-A and certain inhibitory activity against DYRK1A .
    Norharmine
  • HY-162597
    Dyrk1A-IN-9

    		DYRK Neurological Disease
    Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC50: 1.67 μM). L9 shows neuroprotective activity by regulating the expression of Aβ and phosphorylation of Tau protein. Dyrk1A-IN-9 can be used for research of Alzheimer's disease .
    Dyrk1A-IN-9
  • HY-108475
    ProINDY

    		DYRK Cancer
    ProINDY, a prodrug of INDY (HY-108476), is a DYRK1A and DYRK1B inhibitor. ProINDY effectively recovers Xenopus embryos from head malformation induced by Dyrk1A overexpression .
    ProINDY
  • 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 .
    Dyrk1A/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 .
    Dyrk1A/α-synuclein-IN-2
  • HY-144614
    JH-XVII-10

    		DYRK Apoptosis Neurological Disease Cancer
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XVII-10
  • HY-129449
    AnnH31

    		Monoamine Oxidase DYRK Neurological Disease Cancer
    AnnH31 is a Dyrk1A inhibitor (IC50: 81 nM). AnnH31 also inhibits MAO-A with an IC50 of 3.2 μM .
    AnnH31
  • HY-144617
    JH-XIV-68-3

    		DYRK Cancer
    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XIV-68-3
  • HY-144290
    ARN25068

    		GSK-3 DYRK Neurological Disease
    ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
    ARN25068
  • HY-108476
    INDY
    2 Publications Verification

    		 DYRK Cancer
    INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
    INDY
  • HY-142295
    GNF2133

    		DYRK Metabolic Disease
    GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes .
    GNF2133
  • HY-142295A
    GNF2133 hydrochloride

    		DYRK Metabolic Disease
    GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes .
    GNF2133 hydrochloride
  • HY-34222
    7-Deazaguanine

    		DYRK Cancer
    7-Deazaguanine (Compound 1) is a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor. 7-Deazaguanine is promising for research of cancers and Down’s syndrome .
    7-Deazaguanine
  • HY-12838
    RO5454948
    1 Publications Verification

    Mirk-IN-1; DYRK1B/A-IN-1

    		 DYRK Cancer
    Mirk-IN-1 (Dyrk1B/A-IN-1) is a highly efficient and selective inhibitor of Dyrk1B and Dyrk1A, with IC50 values of 68 and 22nM respectively.
    RO5454948
  • HY-146586
    Haspin-IN-1

    		Haspin Kinase CDK DYRK Cancer
    Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC50 of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 221 nM and 916.3 nM, respectively .
    Haspin-IN-1
  • HY-146587
    Haspin-IN-2

    		Haspin Kinase CDK DYRK Cancer
    Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC50 of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 445 nM and 917 nM, respectively .
    Haspin-IN-2
  • HY-110052
    TBCA

    		Casein Kinase Cancer
    TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases .
    TBCA
  • HY-128759
    DYRKs-IN-2

    		DYRK Cancer
    DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity .
    DYRKs-IN-2
  • HY-101298
    Paprotrain
    1 Publications Verification

    		 Kinesin Neurological Disease
    Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
    Paprotrain
  • HY-111380
    EHT 1610
    1 Publications Verification

    		 DYRK Neurological Disease
    EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis - .
    EHT 1610
  • HY-128758
    DYRKs-IN-1

    		DYRK Cancer
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .
    DYRKs-IN-1
  • HY-128758A
    DYRKs-IN-1 hydrochloride

    		DYRK Cancer
    DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .
    DYRKs-IN-1 hydrochloride
  • HY-105309
    GSK-626616
    Maximum Cited Publications
    7 Publications Verification

    		 DYRK Cardiovascular Disease
    GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia .
    GSK-626616
  • HY-77324S
    4-(Trifluoromethyl)aniline-d4

    4-Aminobenzotrifluoride-d4

    		 DYRK Cancer
    4-(Trifluoromethyl)aniline-d4 is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively[1].
    4-(Trifluoromethyl)aniline-d4
  • HY-N2892
    Aristolactam A IIIa

    Aristololactam A IIIa; Sch 546909

    		 DYRK Cardiovascular Disease Cancer
    Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells .
    Aristolactam A IIIa
  • HY-15951
    ML167

    CID44968231; NCGC00188654

    		 CDK DYRK Cancer
    ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B .
    ML167
  • HY-12828A
    KH-CB20

    		CDK DYRK Infection Neurological Disease
    KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM) .
    KH-CB20
  • HY-152183
    FINDY

    		DYRK Neurological Disease
    FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY can inhibit Ser97 autophosphorylation with an IC50 value of 35 μM. FINDY can be used for the research of neurological disorder . FINDY is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FINDY
  • HY-129492
    GNF4877
    1 Publications Verification

    		 DYRK GSK-3 Metabolic Disease
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
    GNF4877
  • HY-144826
    ZDWX-25

    		GSK-3 Neurological Disease
    ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. ZDWX-25 possesses significant cytotoxic activities against SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for researching alzheimer's disease .
    ZDWX-25
  • HY-N12625
    (R)-(+)-O-Demethylbuchenavianine

    		CDK DYRK GSK-3 Cancer
    (R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively .
    (R)-(+)-O-Demethylbuchenavianine
  • HY-163514
    hAChE-IN-8

    		Cholinesterase (ChE) DYRK Neurological Disease
    hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research .
    hAChE-IN-8
  • 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-155723
    Leucettinib-92

    		CDK DYRK Others
    Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3) .
    Leucettinib-92
  • HY-101029
    MBM-55

    		NEKs Apoptosis Cancer
    MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .
    MBM-55
  • HY-15569
    NU6102

    		CDK Cancer
    NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC50 of 1.6 μM), DYRK1A (IC50 of 0.9 μM), PDK1 (IC50 of 0.8 μM) and ROCKII (IC50 of 0.6 μM) .
    NU6102

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