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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 [1].
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 [1].
Dyrk1a Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Dyrk1a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
DYRK1A Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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 [1].
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-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 [1].
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 [1].
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-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) [1].
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-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-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/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/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 [1].
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 [1].
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].
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].
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 [1].
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 [1].
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].
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] .
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) [1].
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[1].
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].
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].
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 [1] .
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) [1] .
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 [1].
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 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].
DYRKtide is a biological active peptide. (Dyrktide is designed as the optimal substrate sequence efficiently phosphorylated by DYRK1A, which is a dual-specificity protein kinase that is thought to be involved in brain development.)
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy [1].
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 [1] .
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 [1].
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.
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 [1] .
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 [1] .
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].
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 [1].
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 [1].
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].
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 [1]. 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.
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) [1].
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 [1].
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 [1].
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 [1].
ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2,CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity [1].
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 [1].
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S 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-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice [1].
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) [1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
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 [1].
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research [1].
CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity [1].
DYRKtide is a biological active peptide. (Dyrktide is designed as the optimal substrate sequence efficiently phosphorylated by DYRK1A, which is a dual-specificity protein kinase that is thought to be involved in brain development.)
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 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].
DYRK1A protein has dual serine/threonine and tyrosine kinase activities. DYRK1A Protein, Human is the recombinant human-derived DYRK1A protein, expressed by E. coli , with tag free. The total length of DYRK1A Protein, Human is 359 a.a., .
DYRK1A protein has dual serine/threonine and tyrosine kinase activities. DYRK1A Protein, Human (His) is the recombinant human-derived DYRK1A protein, expressed by E. coli , with N-6*His labeled tag. The total length of DYRK1A Protein, Human (His) is 359 a.a., .
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].
Dyrk1a Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Dyrk1a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
DYRK1A Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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