PHT-427
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.
PHT-427是Akt和PDPK1的抑制剂，Ki值分别为2.7 μM和5.2 μM。
Akt是一种丝氨酸/苏氨酸特异性蛋白激酶，在多种细胞过程发挥重要作用，包括葡萄糖代谢、凋亡、细胞增殖、转录和细胞迁移等。
在BxPC-3细胞中，PHT-427抑制Akt及其下游底物的功能，IC50值为8.6 ± 0.8 μM。PHT-427减少Akt 中Ser473位点的磷酸化，对Akt的总蛋白水平没有影响。PHT-427以剂量依赖的方式抑制p70S6K和GSK3β[1,2]。
在BxPC-3胰腺癌异种移植的SCID（重症联合免疫缺陷）小鼠中，PHT-427产生明显的抗肿瘤活性，停止肿瘤生长。在NSC肺癌中，PHT-427与厄洛替尼组合使用的抗肿瘤效果大于累计的抗肿瘤效果，在乳腺癌中则与紫杉醇联合使用 [1,2]
参考文献：
1. Meuillet EJ, Zuohe S, Lemos R et al. Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther. 2010 Mar;9(3):706-17.
2. Moses SA, Ali MA, Zuohe S et al. In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT. Cancer Res. 2009 Jun 15;69(12):5073-81.
| Storage | Store at -20°C |
| M.Wt | 409.61 |
| Cas No. | 1191951-57-1 |
| Formula | C20H31N3O2S2 |
| Solubility | insoluble in H2O; ≥20.5 mg/mL in DMSO; ≥51.1 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2 |
| 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。 |
| Description | PHT-427是Akt和PDPK1的抑制剂，Ki值分别为2.7 μM和5.2 μM。 | |||||
| 靶点 | Akt | PDK-1 | ||||
| IC50 | 2.7 μM(Ki) | 5.2 μM(Ki) | ||||
质量控制和MSDS
- 批次:
化学结构
