AZ191
Based on 7 publication(s) in Google Scholar
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 1594092-37-1
- Fòrmula: C24H27N7O
- Peso molecular:429.52
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Chemical Probe Library
HY-L063
-
Anti-Obesity Compound Library
HY-L087
-
Targeted Diversity Library
HY-L099
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Bioactive Compound Library Max
HY-L181
-
Kinase Inhibitor Library Mini
HY-L009M
-
MCE Bioactive Compound Library
HY-L001V
Publications Citing Use of MedChemExpress (MCE) AZ191
More
Actividad biológica
|
DYRK1B |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| COS-1 | IC50 |
0.042 μM
Compound: 19
|
Inhibition of human full length C-terminal c-Myc tagged Dyrk1B phosphorylation overexpressed in monkey COS1 cells after 5 hrs by ELISA
Inhibition of human full length C-terminal c-Myc tagged Dyrk1B phosphorylation overexpressed in monkey COS1 cells after 5 hrs by ELISA
|
[PMID: 25738750] |
| HT-22 | IC50 |
27.8 μM
Compound: 5; AZ191
|
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
|
[PMID: 36876904] |
AZ191 (0.01-60μM; 5 days) inhibits SW872 and SW982 cell lines in dose-dependent manner with IC50s of 3.183 μM and 1.279 μM, respectively[2].
AZ191 (1-5 μM; 48 hours) down-regulates three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SW872, SW982 liposarcoma cells
-
Concentration:0.01, 0.03, 0.1, 0.3, 0.6, 1, 3, 6, 10, 20, 60 μM
-
Incubation Time:5 days
-
Result:Dose-dependent growth inhibition with IC50s of 3.183 μM and 1.279 μM for SW872 and SW982 cell lines, respectively.
-
Cell Line:SW872, SW982 liposarcoma cells
-
Concentration:1, 2, 3, 4, 5 μM
-
Incubation Time:48 hours
-
Result:Down-regulated three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations.
Chemical Information
-
No. CAS 1594092-37-1
-
Appearance Solid
-
Peso molecular 429.52
-
Fòrmula C24H27N7O
-
Color Gray to brownish yellow
-
SMILES
CN1C2=CN=CC=C2C(C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4OC)=NC=C3)=C1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
F-box protein FBXO32 ubiquitinates and stabilizes D-type cyclins to drive cancer progression. [Abstract]2025 Apr 30;16(1):4060. PMID: 40307251 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Biol Res
DYRK1-mediated phosphorylation of endocytic components is required for extracellular lumen expansion in ascidian notochord. [Abstract]2023 Mar 11;56(1):10. PMID: 36899423 -
-
Sci Total Environ
Chronic di(2-ethylhexyl) phthalate exposure at environmental-relevant doses induces osteoporosis by disturbing the differentiation of bone marrow mesenchymal stem cells. [Abstract]2024 Mar 1:914:169918. PMID: 38190899 -
Solvente y solubilidad
DMSO : ≥ 30 mg/mL (69.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Ashford AL, et al. A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288). Biochem J. 2014 Jan 1;457(1):43-56. [Content Brief]
[2]. Chen H, et al. Targeting DYRK1B suppresses the proliferation and migration of liposarcoma cells. Oncotarget. 2017 Nov 28;9(17):13154-13166. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3282 mL | 11.6409 mL | 23.2818 mL | 58.2045 mL |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6564 mL | 11.6409 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL | 5.8205 mL | |
| 15 mM | 0.1552 mL | 0.7761 mL | 1.5521 mL | 3.8803 mL | |
| 20 mM | 0.1164 mL | 0.5820 mL | 1.1641 mL | 2.9102 mL | |
| 25 mM | 0.0931 mL | 0.4656 mL | 0.9313 mL | 2.3282 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7761 mL | 1.9402 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5820 mL | 1.4551 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1641 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9701 mL |
AZ191 Related Classifications
HY-12277 Related Classifications
Powered by Bioz