Find Posaconazole Modulators, Calcitriol Modulators, Cyclosporin A Modulators on Industry Directory, Reliable Manufacturer/Supplier/Factory from China.

Inquiry Basket (0)
Home > Products > Others > Other > AZ191 1594092-37-1

AZ191 1594092-37-1

Product Description

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}

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.

Biological Activity

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 [1] DYRK1A [1] DYRK2 [1]
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: [1]

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)

Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

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
rat Km(6)

Chemical Information

Molecular Weight (MW) 429.52


CAS No. 1594092-37-1

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms N/A

Solubility (25°C) * In vitro DMSO 86 mg/mL (200.22 mM)
Water <1 mg/mL (
Ethanol 1 mg/mL (2.32 mM)

Chemical Name N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine

Contact us if you need more details on AZ191. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about 1594092-37-1 AZ191、1594092-37-1. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Others > Other

Email to this supplier
  • *Subject:
  • To:

  • *Messages:
    Your message must be between 20-8000 characters