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Results for "

DYRK1A+inhibitor

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-142295
    GNF2133
    1 Publications Verification

    		 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 [1].
    GNF2133
  • 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 [1] .
    INDY
  • HY-142295A
    GNF2133 hydrochloride
    1 Publications Verification

    		 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 [1].
    GNF2133 hydrochloride
  • HY-132308
    DYRK1-IN-1
    3 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 [1].
    DYRK1-IN-1
  • HY-147066
    Dyrk1A-IN-4

    		DYRK Cancer
    Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC50s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC50 of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma [1].
    Dyrk1A-IN-4
  • 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. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research [1].
    Dyrk1A-IN-5
  • 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 [1].
    7-Deazaguanine
  • 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 [1].
    Dyrk1A-IN-3
  • HY-176723
    RD0392

    		DYRK Neurological Disease
    RD0392 (Compound 5) is a competitive tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50=1.3 nM). RD0392 is promising for research of neurodegenerative diseases like Alzheimer’s [1].
    RD0392
  • HY-176402
    Dyrk1A-IN-13

    		DYRK NO Synthase Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Dyrk1A-IN-13 (Compound 1) is a DYRK1A inhibitor (IC50: 41 nM). Dyrk1A-IN-13 reduces LPS-induced NO production and has antioxidant and anti-inflammatory activities. Dyrk1A-IN-13 can be used in the research of Alzheimer's disease, cancer and diabetes [1].
    Dyrk1A-IN-13
  • HY-179177
    AO-365/43472821

    		DYRK CDK Tau Protein Amyloid-β Neurological Disease
    AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC50 = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau (pSer396)/tau and Aβ1-42 protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease [1].
    AO-365/43472821
  • 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 [1].
    Aristolactam A IIIa
  • 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 [1].
    JH-XVII-10
  • 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 [1].
    ProINDY
  • 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 [1].
    Aristolactam BIII
  • 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 [1].
    Dyrk1A-IN-11
  • 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 inhibits cell viability of HeLa, PC12 and SH-SY5Y cells [1].
    AnnH31
  • 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 [1].
    Dyrk1A-IN-2
  • 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 [1].
    Dyrk1A-IN-10
  • 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 [1].
    Dyrk1A-IN-9
  • 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 [1].
    Dyrk1A/B-IN-1
  • HY-108476R
    INDY (Standard)

    		Reference Standards DYRK Cancer
    INDY (Standard) is the analytical standard of INDY (HY-108476). This product is intended for research and analytical applications. 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 [1] .
    INDY (Standard)
  • HY-179600
    Dyrk1A-IN-16

    		DYRK EGFR Neurological Disease Cancer
    Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research [1].
    Dyrk1A-IN-16
  • HY-179599
    Dyrk1A-IN-15

    		DYRK EGFR Neurological Disease Cancer
    Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research [1].
    Dyrk1A-IN-15

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