YM201636
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
YM201636是一种有效的细胞可透过的哺乳动物III类磷脂酰肌醇磷酸激酶PIKfyve的选择性抑制剂,IC50值为33 nM[1].
吡啶并嘧啶类物质YM201636是一种小分子的PIKfyve抑制剂.在体外试验中,该物质可抑制PIKfyve,IC50值为33 nM,对酵母中的同源PIKfyve无抑制能力.该物质可抑制PtdIns3P p110α和Iα型PtdInsP激酶,IC50值分别为3 μM和大于2 μM.IIγ型PtdInsP激酶对YM201636不敏感.在血清饥饿的NIH3T3细胞中,YM201636在800 nM浓度下可抑制80%的PtdIns (3, 5) P2产生.YM201636对MEFs\MDCK\MCF10A\COS7和NIH3T3细胞的急性治疗会导致大泡状结构的形成.除此之外,YM201636可也抑制胰岛素依赖的I类PI3K激活,降低Akt磷酸化和GLUT4细胞表面易位[1,2].
参考文献:
[1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170.
[2] Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 467.48 |
Cas No. | 371942-69-7 |
Formula | C25H21N7O3 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥11.68 mg/mL in DMSO |
Chemical Name | 6-amino-N-[3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenyl]pyridine-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1, 2]: | |
细胞系 |
小鼠3T3L1脂肪细胞,NIH3T3细胞 |
溶解方法 |
该化合物在DMSO中的溶解度>11.7mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0-4 μM给药30分钟或800 nM给药2h |
应用 |
在小鼠3T3L1脂肪细胞中,YM201636以剂量依赖性方式显著抑制基础和胰岛素激活的2DG摄取。 YM201636(160nM)几乎完全抑制了胰岛素效应,在54±4nM下具有50%的抑制作用。 800nM的YM201636产生细胞表面HA-GLUT4-eGFP积累的45%抑制和Akt-Ser473磷酸化的55%抑制。在NIH3T3细胞中,800nM的YM201636将PtdIns(3,5)P2产量降低80%。YM201636通过影响PIKfyve和PtdIns(3,5)P2生产诱导囊泡表型。 |
References: [1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170. [2]. Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570. |
Description | YM201636是一种PIKfyve的选择性抑制剂,IC50值为33 nM. | |||||
靶点 | PIKfyve | p110α | ||||
IC50 | 33 nM | 3.3 μM |
质量控制和MSDS
- 批次: