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Chemical Structure| 1594092-37-1 Chemical Structure| 1594092-37-1

Structure of AZ191
CAS No.: 1594092-37-1

Chemical Structure| 1594092-37-1

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AZ 191 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.

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Product Details of AZ191

CAS No. :1594092-37-1
Formula : C24H27N7O
M.W : 429.52
SMILES Code : CN1C=C(C2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2)C5=C1C=NC=C5
MDL No. :MFCD28015098
InChI Key :ZYVXTMKTGDARKR-UHFFFAOYSA-N
Pubchem ID :72716071

Safety of AZ191

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZ191

RTK

Isoform Comparison

Biological Activity

Target
  • DYRK1

    DYRK1A, IC50:88 nM

    DYRK1B, IC50:17 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Huh7 cells 1 μM 24 h Evaluate the effect of AZ191 on the cell cycle distribution of Huh7 cells PMC7838256
RPE-1 10 μM 1 h To investigate the effect of AZ191 on rDNA DSB-induced transcriptional silencing. Results showed that AZ191 pretreatment led to failure of nucleolar transcriptional silencing. PMC7897492
HeLa 10 μM 1 h To investigate the effect of AZ191 on rDNA DSB-induced transcriptional silencing. Results showed that AZ191 pretreatment led to failure of nucleolar transcriptional silencing. PMC7897492
U2OS 10 μM 1 h To investigate the effect of AZ191 on rDNA DSB-induced transcriptional silencing. Results showed that AZ191 pretreatment led to failure of nucleolar transcriptional silencing. PMC7897492
HEK293 cells 10 μM 10 min AZ191 failed to inhibit DYRK1B-dependent mTOR-Ser2448 phosphorylation PMC8803348
MKpc4 cells 1 µM 4 days To evaluate the effect of AZ191 on cell proliferation, results showed that AZ191 treatment increased the percentage of BrDU-positive cells. PMC11420735
Ciona savignyi embryos 40 µM 4-8 h To inhibit DYRK1 kinase activity and observe its effects on notochord development and lumenogenesis in ascidian Ciona savignyi. Results showed that AZ191 treatment significantly delayed tail elongation and lumen expansion. PMC10047359
DU145 prostate cancer cells 3–10 µM 1 h AZ191 inhibited p27Kip1 nuclear expression, indicating cells were not quiescent PMC7385110

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous xenograft tumor model Intraperitoneal injection 50 mg/kg Six injections Evaluate the inhibitory effect of AZ191 on HCC cell growth PMC7838256
Chick embryos Embryonic chick spinal cord Injection 600 µg Single injection, lasting 48 hours AZ191 increases the numbers of ventral progenitors and MNs by inhibiting endogenous Dyrk1B kinase activity PMC10830675
Mice KPC mouse model Intraperitoneal injection 5 mg/kg Twice weekly, continuous treatment To evaluate the effect of AZ191 alone or in combination with other drugs, results showed that AZ191 combination therapy significantly extended the survival of mice. PMC11420735

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.64mL

2.33mL

1.16mL

23.28mL

4.66mL

2.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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