化合物AZ191 T6257
面议
- TargetMol
- 生产商
- 进口
- 美国
- 现货
- 全国
- 7
- 1
Product IntroductionBioactivity英文名: AZ191描述: AZ191 是特异性 DYRK1B 抑制剂。它对 DYRK1B 的特异性分别是 DYRK1A 和 DYRK2 的 5 倍和 110 倍。激酶实验: Bi
AI问答
配套的仪器设备？
可以搭配的相关耗材试剂？
耗材描述
Product Introduction
Bioactivity
英文名: AZ191
描述: AZ191 是特异性 DYRK1B 抑制剂。它对 DYRK1B 的特异性分别是 DYRK1A 和 DYRK2 的 5 倍和 110 倍。
激酶实验: Biochemical Binding Affinity – HTRF Assay: The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.
体外活性: 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. [1]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 1 mg/mL (2.32 mM)
DMSO : 79 mg/mL (183.9 mM)
关键字: Inhibitor | Dual specificity tyrosine regulated kinase | Dual specificity tyrosine phosphorylation regulated kinase | inhibit | AZ191 | DYRK | AZ 191 | AZ-191
相关产品: Harmine | LDN-192960 | ML167 | GNF4877 | DYRKs-IN-2 | AnnH31 | GSK-626616 | INDY | ARN25068 | CK2/ERK8-IN-1
相关库: Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
Bioactivity
英文名: AZ191
描述: AZ191 是特异性 DYRK1B 抑制剂。它对 DYRK1B 的特异性分别是 DYRK1A 和 DYRK2 的 5 倍和 110 倍。
激酶实验: Biochemical Binding Affinity – HTRF Assay: The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.
体外活性: 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. [1]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 1 mg/mL (2.32 mM)
DMSO : 79 mg/mL (183.9 mM)
关键字: Inhibitor | Dual specificity tyrosine regulated kinase | Dual specificity tyrosine phosphorylation regulated kinase | inhibit | AZ191 | DYRK | AZ 191 | AZ-191
相关产品: Harmine | LDN-192960 | ML167 | GNF4877 | DYRKs-IN-2 | AnnH31 | GSK-626616 | INDY | ARN25068 | CK2/ERK8-IN-1
相关库: Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
猜你喜欢
感兴趣产品