DYRK
Inhibitory Selectivity
Isoform-specific Inhibitors
DYRK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7338 |
AZ191AZ191 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. |
In (e), quiescent cells were left untreated or treated for 30 min with 10 nM R1881, in the absence or presence of the DYRK 1B inhibitor AZ191, which was added (1 μM) 15 min before hormonal stimulation. Control cells in right panel were treated with the inhibitor alone. In left panels, lysate proteins were immunoprecipitated with anti-DYRK 1B antibody. Immune complexes were analyzed for DYRK 1B activity using MBP as a substrate. DYRK 1B levels in immune complexes were detected by immunoblot with anti-DYRK 1B antibody. In right panels, lysate proteins were analyzed by western blot, using antibodies against the indicated proteins. |
|
| S7327 |
ID-8ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture. |
||
| S3817 |
Harmine hydrochlorideHarmine (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) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
||
| S3406New |
LDN-192960LDN-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7338 |
AZ191AZ191 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. |
In (e), quiescent cells were left untreated or treated for 30 min with 10 nM R1881, in the absence or presence of the DYRK 1B inhibitor AZ191, which was added (1 μM) 15 min before hormonal stimulation. Control cells in right panel were treated with the inhibitor alone. In left panels, lysate proteins were immunoprecipitated with anti-DYRK 1B antibody. Immune complexes were analyzed for DYRK 1B activity using MBP as a substrate. DYRK 1B levels in immune complexes were detected by immunoblot with anti-DYRK 1B antibody. In right panels, lysate proteins were analyzed by western blot, using antibodies against the indicated proteins. |
|
| S7327 |
ID-8ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture. |
||
| S3817 |
Harmine hydrochlorideHarmine (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) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
||
| S3406New |
LDN-192960LDN-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. |
