A66
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.
A66是p110α的强效选择性抑制剂，IC50为32 nM。
P110α是I类磷脂酰肌醇-4,5-二磷酸3-激酶的催化亚基，该酶含有一个85 kDa的调节亚基和110kDa的催化亚基。
在某些含有PIK3CA突变H1047R和高水平p110a的细胞系中，A66抑制Akt/PKB的磷酸化[1]。在C2C12成肌细胞和3T3-L1脂肪细胞中，A66可减少S6K上Thr389位点的磷酸化，该磷酸化是S6K激酶活化的标志，并可阻止慢性胰岛素诱导的IRS的下调[2]。
该化合物被广泛应用在各种动物模型来研究PI3K的作用。例如，在体内异种移植模型中，A66抑制p110α，可以减少某些细胞系的肿瘤生长[1]。A66对p110α的慢性药理学抑制可以阻止持续代谢应激诱导的胰岛素抗性[2]。在移植原发肿瘤乳房脂肪垫的无胸腺小鼠模型中，A66显著减少肿瘤生长[3]。
参考文献：
1. Jamieson S, Flanagan JU, Kolekar S, Buchanan C, Kendall JD, Lee WJ, et al. A drug targeting only p110alpha can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J 2011,438:53-62.
2. Foukas LC, Bilanges B, Bettedi L, Pearce W, Ali K, Sancho S, et al. Long-term p110alpha PI3K inactivation exerts a beneficial effect on metabolism. EMBO Mol Med 2013,5:563-571.
3. Utermark T, Rao T, Cheng H, Wang Q, Lee SH, Wang ZC, et al. The p110alpha and p110beta isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis. Genes Dev 2012,26:1573-1586.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 393.53 |
| Cas No. | 1166227-08-2 |
| Formula | C17H23N5O2S2 |
| Synonyms | A 66; A-66 |
| Solubility | insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming |
| Chemical Name | (2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CSC(=N3)C(C)(C)C |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
