| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| Y409040-1ml |
1ml |
现货  |
|
| 英文别名 | 3-Pyridinecarboxamide, 6-amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | YM201636 |
| 生化机理 | YM201636 是一种选择性 PIKfyve 抑制剂，IC50 为 33 nM，对 p110α 的作用较弱，对酵母同源物 Fabl 不敏感。YM-201636 通过诱导自噬抑制肝癌的生长。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
YM201636是一种选择性的PIKfyve抑制剂，IC50为33 nM，对p110α作用效果稍弱，对Fabl(酵母同源基因)不敏感。YM-201636 可通过诱导自噬来抑制肝癌的生长。 Information YM201636 is a selectivePIKfyveinhibitor withIC50of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction ofautophagy. YM201636 potently inhibits mammalian PIKfyve with an IC50 of 33 nM but not yeast orthologue Fab1 with an IC50 of >5 μM, exhibiting around 100-fold selectivity for PtdIns3P p110α with an IC50 of 3 μM. YM201636 (0.8 μM) significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells followed by serum stimulation with no effect on serum-stimulated protein kinase B (PKB) Ser 473 phosphorylation. YM-201636 reversibly impairs endosomal trafficking in NIH3T3 cells by blocking PIKfyve and PtdIns(3,5)P2 production, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 (0.8 μM) also significantly reduces retroviruses budding from cells by 80%, apparently through interfering with the endosomal sorting complex required for transport (ESCRT) machinery. In 3T3L1 adipocytes, YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake with an IC50 of 54 nM, with almost complete inhibition at doses as low as 160 nM. YM-201636 (0.1 μM) has also been shown to completely block insulin-dependent activation of class IA PI 3-kinase. Although not involved in NPM-ALK-dependent proliferation and migration, YM201636 (0.4 μM) strongly reduces invasive capacities of NPM-ALK-expressing cells and their capacity to degrade the extracellular matrix. YM201636 treatment blocks the continuous recycling of junctional proteins claudin-1 and claudin-2 in MDCK cells, leading to the intracellular accumulation and delay of epithelial barrier formation. In vivo
cell lines： Concentrations： Incubation Time： Powder Purity:≥98% |
| Isomeric SMILES | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N |
|---|---|
| PubChem CID | 9956222 |
| 分子量 | 467.48 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 94 mg/mL (200.45 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
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