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DYRK

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Catalog No. Product Name Information Product Use Citations Product Validations
S7338 AZ191 AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
Nucleic Acids Res, 2021, gkaa1290
Cell Death Dis, 2021, 12(1):125
Cell Death Dis, 2021, 12(1):125
S7327 ID-8 ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.
Cell Chem Biol, 2022, 29(9):1368-1380.e5
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
Cancers (Basel), 2022, 14(2)326
S3406 LDN-192960 LDN-192960 (Compd 1) is a potent inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50 of 10 nM and 48 nM, respectively.
Colloids Surf B Biointerfaces, 2022, 209(Pt 1):112182
E2668 Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active inhibitor of CDC-like kinase (CLK) and a DYRK (dual-specificity tyrosine kinase) that targets mRNA splicing and is optimized for Wnt pathway inhibition. Cirtuvivint inhibits serine and arginine-rich splicing factor (SRSF) phosphorylation and disrupts spliceosome activity. Cirtuvivint can be used for solid tumor research.
E0779 Paprotrain 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.
S8395 INDY INDY, a benzothiazole derivative is a potent and ATP-competitive inhibitor of Dyrk1A and Dyrk1B with an IC50 value of 0.24 μM and Ki value of 0.18 μM, respectively. INDY diminishes the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.
E2853 GSK626616 GSK-626616 is a dual-specificity tyrosine-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM which is a potential therapy for the treatment of anemia.
S7338 AZ191 AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
Nucleic Acids Res, 2021, gkaa1290
Cell Death Dis, 2021, 12(1):125
Cell Death Dis, 2021, 12(1):125
S7327 ID-8 ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.
Cell Chem Biol, 2022, 29(9):1368-1380.e5
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
Cancers (Basel), 2022, 14(2)326
S3406 LDN-192960 LDN-192960 (Compd 1) is a potent inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50 of 10 nM and 48 nM, respectively.
Colloids Surf B Biointerfaces, 2022, 209(Pt 1):112182
E2668 Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active inhibitor of CDC-like kinase (CLK) and a DYRK (dual-specificity tyrosine kinase) that targets mRNA splicing and is optimized for Wnt pathway inhibition. Cirtuvivint inhibits serine and arginine-rich splicing factor (SRSF) phosphorylation and disrupts spliceosome activity. Cirtuvivint can be used for solid tumor research.
E0779 Paprotrain 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.
S8395 INDY INDY, a benzothiazole derivative is a potent and ATP-competitive inhibitor of Dyrk1A and Dyrk1B with an IC50 value of 0.24 μM and Ki value of 0.18 μM, respectively. INDY diminishes the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.
E2853 GSK626616 GSK-626616 is a dual-specificity tyrosine-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM which is a potential therapy for the treatment of anemia.

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Tags: DYRK inhibitor|DYRK agonist|DYRK activator|DYRK inducer|DYRK antagonist|DYRK signaling pathway|DYRK assay kit