PHT-427 | Akt Inhibitor XIV | Akt Inhibitor | AmBeed-信号通路专用抑制剂

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PHT-427 99%+

货号：A160471 同义名： Akt Inhibitor XIV;CS-0223 产品仅供科研

PHT-427 is dual inhibitor of Akt and PDPK1 with Ki of 2.7 μM and 5.2 μM, respectively, targeting PH domains of Akt and PDPK1.

PHT-427 化学结构
CAS号：1191951-57-1

PHT-427 3D分子结构
CAS号：1191951-57-1

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PHT-427 纯度/质量文件

货号：A160471 标准纯度：99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

PDK 亚型比较
Akt 亚型比较

产品名称	PDK1 ↓ ↑	其他靶点	纯度
OSU-03012	++ PDK-1, IC50: 5 μM		99%+
BX-912	+++ PDK-1, IC50: 12 nM	PKA	99%+
GSK2334470	+++ PDK-1, IC50: 10 nM		99%+
BX795	++++ PDK-1, IC50: 6 nM	c-Kit	99%+
PHT-427	+ PDK1, Ki: 5.2 μM	Akt	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Akt ↓ ↑	Akt1 ↓ ↑	Akt2 ↓ ↑	Akt3 ↓ ↑	其他靶点	纯度
Honokiol	✔				MEK	98%
PF-04691502	++++ P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM					99%+
PHT-427	+ Akt, Ki: 2.7 μM					99%+
Deguelin	✔				PI3K	99%+
TIC10 isomer	✔				ERK	98+%
Perifosine	+ Akt, IC50: 4.7 μM					98%
Miltefosine	✔				PI3K,PKC	98%
Triciribine	+ Akt, IC50: 130 nM					99%+
Uprosertib		+ Akt1, IC50: 180 nM	+ Akt2, IC50: 328 nM	++ Akt3, IC50: 38 nM		99%+
Afuresertib		++++ Akt1, Ki: 0.08 nM	++++ Akt2, Ki: 2 nM	++++ Akt3, Ki: 2.6 nM		99%+
Miransertib		++++ Akt1, IC50: 5 nM	++++ Akt2, IC50: 4.5 nM	++ Akt3, IC50: 16 nM		98+%
GSK-690693		++++ Akt1, IC50: 2 nM	+++ Akt2, IC50: 13 nM	+++ Akt3, IC50: 9 nM		99%+
AT7867		++ Akt1, IC50: 32 nM	++ Akt2, IC50: 17 nM	++ Akt3, IC50: 47 nM	PKA	99%+
AKT inhibitor VIII		++ Akt1, IC50: 58 nM	+ Akt2, IC50: 210 nM	+ Akt3, IC50: 2119 nM		98+%
MK-2206 2HCl		+++ Akt1, IC50: 8 nM	+++ Akt2, IC50: 12 nM	+ Akt3, IC50: 65 nM		99%+
Ipatasertib		++++ Akt1, IC50: 5 nM	++ Akt2, IC50: 18 nM	+++ Akt3, IC50: 8 nM		99%+
AT13148		++ Akt1, IC50: 38 nM	+ Akt2, IC50: 402 nM	++ Akt3, IC50: 50 nM	PKA	98+%
Capivasertib		++++ Akt1, IC50: 3 nM	+++ Akt2, IC50: 8 nM	+++ Akt3, IC50: 8 nM		99%+
A-674563 HCl		+++ Akt1, Ki: 11 nM			PKA	98%
CCT128930			+++ Akt2, IC50: 6 nM		PKA	98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

PHT-427 生物活性

靶点

PDK1

PDK1, Ki:5.2 μM
Akt

Akt, Ki:2.7 μM
Akt

Akt, Ki:2.7 μM

描述

Phosphatidylinositol 3-kinase (PIK3)/PtdIns dependent protein kinase-1(PDPK1)/Akt signaling plays a critical role in activating proliferation and survival pathways within cancer cells. PHT-427 is a compound designed to bind to the pleckstrin homology (PH) binding domain of signaling molecules. PHT-427 itself (C-12 chain) bound with the highest affinity to the PH domains of both PDPK1 and Akt. PHT-427 inhibited Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. The Ki values of PHT-427 are 2.7 and 5.2 µM towards Akt and PDPK1 respectively. RPPA studies in PC-3 prostate cancer cells showed that PHT-427 caused a reduction in phospho-Thr³⁰⁸-Akt, and also in phospho-Ser²⁴¹-PDPK1 and its downstream targets, phospho-Ser⁶⁵⁷-PKC and total SGK1. In vivo studies in mice with BxPC-3 and MiaPaCa-2 xenografts treated with a 200 mg/kg dose of PHT-427 showed a decrease in phospho-Ser⁴⁷³-AKT, phospho-Thr³⁰⁸-Akt, phospho-Ser²⁴¹-PDPK1 and in the PDKP1-specific downstream target phospho-Ser²²¹-RSK^[5].

PHT-427 动物研究

Dose	Mice: 200 mg/kg^[3] (p.o.); 10 mg/kg^[4] (i.p.)
Administration	p.o., i.p.

PHT-427 参考文献

[1]Meuillet EJ, Zuohe S, et al. Molecular pharmacology and antitumor activity of PHT-427 a novel AKT/PDPK1 pleckstrin homology domain inhibitor. Mol Cancer Ther, 2010, 9(3), 706-717.

[2]Moses SA, Ali MA, 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.

[3]Madhunapantula SV, Mosca PJ, et al. The Akt signaling pathway: an emerging therapeutic target in malignant melanoma. Cancer Biol Ther. 2011 Dec 15;12(12):1032-49.

[4]Lucero-Acuña A, Jeffery JJ, et al. Nanoparticle delivery of an AKT/PDK1 inhibitor improves the therapeutic effect in pancreatic cancer. Int J Nanomedicine. 2014 Dec 3;9:5653-65.

[5]Meuillet EJ, Zuohe S, Lemos R, Ihle N, Kingston J, Watkins R, Moses SA, Zhang S, Du-Cuny L, Herbst R, Jacoby JJ, Zhou LL, Ahad AM, Mash EA, Kirkpatrick DL, Powis G. 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. doi: 10.1158/1535-7163.MCT-09-0985. Epub 2010 Mar 2. PMID: 20197390; PMCID: PMC2837366.

PHT-427 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.41mL

4.88mL

2.44mL

PHT-427 技术信息

CAS号	1191951-57-1
分子式	C₂₀H₃₁N₃O₂S₂
分子量	409.609

别名	Akt Inhibitor XIV;CS-0223
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(61.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

5% DMSO+95% Corn oil 5 mg/mL

PHT-427 99%+

PHT-427 纯度/质量文件

全球学术期刊中引用的产品

PHT-427 生物活性

PHT-427 动物研究

PHT-427 参考文献

PHT-427 实验方案

PHT-427 技术信息

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PHT-427 99%+

PHT-427 纯度/质量文件

全球学术期刊中引用的产品

PHT-427 生物活性

PHT-427 动物研究

PHT-427 参考文献

PHT-427 实验方案

PHT-427 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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