YM201636
YM201636
CAS: 371942-69-7
Molecular Formula: C25H21N7O3
YM201636 - Names and Identifiers
| Name | YM201636 |
| Synonyms | CS-335 YM201636 YM 201636 |
| CAS | 371942-69-7 |
YM201636 - Physico-chemical Properties
| Molecular Formula | C25H21N7O3 |
| Molar Mass | 467.48 |
| Density | 1.446 |
| Melting Point | >226°C (dec.) |
| Solubility | DMSO (Slightly), Methanol (Very Slightly) |
| Appearance | Solid |
| Color | Pale Beige to Light Beige |
| Storage Condition | -20°C Freezer |
| In vitro study | YM201636 effectively inhibited mammalian PIKfyve with IC50 of 33 nM, but had little effect on the yeast orthologous gene Fab1 with IC50 >5 μm. When it acted on PtdIns3P p110α, the selectivity was about 100 times, the IC50 was 3 μm. 0.8 μm YM201636 significantly reduced PtdIns(3,5)P2 production by 80% in NIH3T3 cells treated with serum starvation, followed by stimulation with serum, there was no effect on serum-stimulated protein kinase B (PKB) phosphorylation at the Ser 473 site. YM-201636 acts on NIH3T3 cells to reversibly impair endosomal trafficking by inhibiting PIKfyve and PtdIns(3,5)P2 production. 0.8 μm YM-201636 significantly reduced cellular reverse transcription by Virus, down to 80%, by interacting with the complex transport (ESCRT) mechanism required for intracellular sorting. YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake in 3T3L1 adipocytes at an IC50 of 54 nM and is completely inhibited at a dose of 160 nM. 0.1 μm YM-201636 completely inhibited the activation of insulin-dependent type IA PI3K. While having no effect on NPM-ALK-dependent proliferation and migration, 0.4 μm YM201636 strongly reduced the ability of cells expressing NPM-ALK to invade and degrade the extracellular matrix. Treatment of MDCK Cells with YM201636 inhibited the continuous recirculation of gap junction proteins Claudin-1 and Claudin-2, resulting in intracellular accumulation and also delayed the formation of the epithelial barrier. YM201636 effectively inhibited mammalian PIKfyve with an IC50 of 33 nM, but had little effect on the yeast orthologous gene Fab1 with an IC50 >5 μm when acting on PtdIns3P p110α, the selectivity was approximately 100-fold and the IC50 was 3 μm. 0.8 μm YM201636 significantly reduced PtdIns(3,5)P 2 production by 80% in NIH3T3 cells treated with serum starvation, and then stimulated with serum on serum-stimulated protein kinase B (PKB) phosphorylation at the Ser 473 site had no effect. YM-201636 action on NIH3T3 cells reversibly impairs endosomal transport by inhibiting PIKfyve and PtdIns(3,5)P 2 production. 0.8 μm YM-201636 significantly reduced cellular reverse transcription by Virus, down to 80%, by interacting with the complex transport (ESCRT) mechanism required for intracellular sorting. YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake in 3T3L1 adipocytes at an IC50 of 54 nM and is completely inhibited at a dose of 160 nM. 0.1 μm YM-201636 completely inhibited the activation of insulin-dependent type IA PI3K. While having no effect on NPM-ALK-dependent proliferation and migration, 0.4 μm YM201636 strongly reduced the ability of cells expressing NPM-ALK to invade and degrade the extracellular matrix. Treatment of MDCK Cells with YM201636 inhibited the continuous recirculation of gap junction proteins Claudin-1 and Claudin-2, resulting in intracellular accumulation and also delayed the formation of the epithelial barrier. |
YM201636 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.139 ml | 10.696 ml | 21.391 ml |
| 5 mM | 0.428 ml | 2.139 ml | 4.278 ml |
| 10 mM | 0.214 ml | 1.07 ml | 2.139 ml |
| 5 mM | 0.043 ml | 0.214 ml | 0.428 ml |
Last Update：2024-01-02 23:10:35
YM201636 - Reference Information
| biological activity | YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, slightly weaker effect on p110α and insensitive to Fabl (yeast homologous gene). YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, which has a slightly weaker effect on p110α and is not sensitive to Fabl (yeast homologous gene). YM-201636 can inhibit the growth of liver cancer by inducing autophagy. |
| in vitro study | YM201636 effectively inhibit mammalian PIKfyve,IC50 is 33 nM, but it has little effect on yeast orthologous gene Fab1, IC50 >5 μM, when acting on PtdIns3P p110α, the selectivity is about 100 times, IC50 is 3 μM. 0.8 μM YM201636 significantly reduced PtdIns(3,5)P2 production by 80% on NIH3T3 cells starved by serum. Subsequently, serum stimulation had no effect on phosphorylation of serum-stimulated protein kinase B (PKB) at Ser 473 site. YM-201636 acts on NIH3T3 cells to reversibly damage endosomal transport by inhibiting PIKfyve and PtdIns(3,5)P2 production. 0.8 μM YM-201636 significantly reduces cellular retroviruses by 80% through interaction with complex transport (ESCRT) mechanisms required for intracellular sorting. YM-201636 acts on 3T3L1 adipocytes to inhibit the absorption of basic and insulin-activated 2-deoxyglucose with an IC50 of 54 nM, which is completely inhibited when treated at a dose of 160 nM. 0.1 μM YM-201636 completely inhibit the activation of insulin-dependent type IA PI3K. Although it has no effect on NPM-ALK-dependent proliferation and migration, 0.4 μM YM201636 strongly reduce the invasion ability of NPM-ALK expressing cells and also reduce the ability to degrade extracellular matrix. YM201636 treatment of MDCK cells inhibits continuous recycling of gap junction protein Claudin-1 and Claudin-2, resulting in intracellular accumulation and delaying the formation of epithelial barrier. YM201636 effectively inhibits mammalian PIKfyve,IC50 is 33 nM, but it has little effect on yeast orthologous gene Fab1, IC50 >5 μM, when it acts on PtdIns3P p110α, the selectivity is about 100 times, IC50 is 3 μM. 0.8 μM YM201636 significantly reduced the production of PtdIns(3,5)P 2 by 80% on NIH3T3 cells starved by serum, and then stimulated by serum had no effect on phosphorylation of serum-stimulated protein kinase B (PKB) at Ser 473 site. YM-201636 acts on NIH3T3 cells to reversibly damage endosomal transport by inhibiting PIKfyve and PtdIns(3,5)P 2 production. 0.8 μM YM-201636 significantly reduces cellular retroviruses by 80% through interaction with complex transport (ESCRT) mechanisms required for intracellular sorting. YM-201636 acts on 3T3L1 adipocytes to inhibit the absorption of basic and insulin-activated 2-deoxyglucose with an IC50 of 54 nM, which is completely inhibited when treated at a dose of 160 nM. 0.1 μM YM-201636 completely inhibit the activation of insulin-dependent type IA PI3K. Although it has no effect on NPM-ALK-dependent proliferation and migration, 0.4 μM YM201636 strongly reduce the invasion ability of NPM-ALK expressing cells and also reduce the ability to degrade extracellular matrix. YM201636 treatment of MDCK cells inhibits continuous recycling of gap junction protein Claudin-1 and Claudin-2, resulting in intracellular accumulation and delaying the formation of epithelial barrier. |
| target | TargetValue PIKfyve (Cell-free say) 33 nM p110α (Cell-free say) 3.3 μM |
| Target | Value |
| PIKfyve (Cell-free assay) | 33 nM |
| p110α (Cell-free assay) | 3.3 μM |
Last Update：2024-04-09 21:11:58
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Spot supply
Product Name: YM201636 Visit Supplier Webpage Request for quotationCAS: 371942-69-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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