|N-(2-甲氧基-4-(4-甲基哌嗪-1-基)苯基)-4-(1-甲基-1H-吡咯并[2,3-c]吡啶-3-基)嘧啶-2-胺|CsnPharm

CAS No.: 1594092-37-1

AZ191 Catalog No. CSN15862

Synonyms: Az 191

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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实验方案

技术信息

生物活性

描述The DYRKs (dual-specificity tyrosine phosphorylation-regulated kinases) are an evolutionarily conserved family of protein kinases that are found within the CMGC group^[3].DYRKs contain a characteristic tyrosine-X-tyrosine (Y-X-Y) residue motif in their activation loop. Phosphorylation of the second tyrosine residue is critical for kinase activity^[4]. AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM. Using in vitro kinase assays, phospho-specific immunoblot analysis and MS in conjunction with AZ191, DYRK1B phosphorylates CCND1 at Thr(286), not Thr(288), in vitro and in cells. In HEK (human embryonic kidney)-293 and PANC-1 cells (which exhibit DYRK1B amplification) DYRK1B drives Thr(286) phosphorylation and proteasome-dependent turnover of CCND1 and this is abolished by AZ191 or DYRK1B RNAi.^[5]. AZ191 inhibited liposarcoma cell growth, decreased cell motility, and induced apoptosis. Moreover, combined AZ191 with doxorubicin demonstrated an increased anti-cancer effect on liposarcoma cells^[6]. Mean inhibitory concentrations (EC50) of 0.98 ± 0.08 μM/SC84227, 0.60 ± 0.02 μM/SC97202, 6.26 ± 1.64 μM/SC97208, 0.71 ± 0.019 μM/Harmine and 0.63 ± 0.23 μM/AZ-191 were determined with human cytomegalovirus strain AD169-GFP for the infection of primary human fibroblasts^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00739362	Electric Stimulation Therapy ... more >> Obesity Weight Loss Eating Collapse <<	Phase 2	Recruiting	January 30, 2025	United States, Arizona ... more >> NIDDK, Phoenix Recruiting Phoenix, Arizona, United States, 85014 Contact: Marci Gluck, Ph.D. 602-200-5312 gmarci@mail.nih.gov Collapse <<
NCT03243305	Contraception	Phase 3	Active, not recruiting	December 2018	-

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3282 mL
- 11.6410 mL
- 23.2819 mL
- 5 mM
- 0.4656 mL
- 2.3282 mL
- 4.6564 mL
- 10 mM
- 0.2328 mL
- 1.1641 mL
- 2.3282 mL

技术信息

CAS号

1594092-37-1

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27N7O

运输

蓝冰

分子量

429.52

别名

Az 191

溶解度

DMSO	85.0 mg/mL (197.9 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.3 mM)

动物实验配方

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AZ191 Catalog No. CSN15862

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