Molecular Weight: 429.52 AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
|Description||AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.|
|Targets||Dyrk1B ||DYRK1A ||DYRK2 |
|IC50||17 nM||88 nM||1890 nM|
|In vitro||AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression.|
|In vivo|| |
Protocol(Only for Reference)
Kinase Assay: 
|In vitro DYRK kinase assay||EGFP–DYRK1A, EGFP–DYRK1B or EGFP–DYRK2 was immunoprecipitated from whole-cell lysate and pre-incubated in the absence or presence of various concentrations of AZ191 or harmine for 5 min at room temperature (20°C) and then assayed for kinase activity by incubating with 50 μM Woodtide, with two additional lysine residues attached to the N-terminus to allow it to bind to P81 paper (KKSSCYVDRKIYTYIQSRFY), 50 mM Tris/HCl (pH 7.5), 0.1 mM EGTA, 0.1% 2-mercaptoethanol, 10 mM MgCl2 and 0.1 mM [γ-32P]ATP in a total volume of 50 μl for 25 min at 30°C.|
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
|Body Surface Area (m2)||0.6||0.5||0.24||0.15||0.05||0.025||0.02||0.007|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×||mouse Km(3)||= 11.2 mg/kg|
|Molecular Weight (MW)||429.52|
|Storage||3 years -20℃Powder|
|6 months-80℃in solvent (DMSO, water, etc.)|
|Solubility (25°C) *||In vitro||DMSO||86 mg/mL (200.22 mM)|
|Water||<1 mg/mL (|
|Ethanol||1 mg/mL (2.32 mM)|
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