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PIP3 Antagonist II, DM-PIT-1-CAS 701947-53-7-Calbiochem

品牌
Sigma-Aldrich
CAS
701947-53-7
货号
524619
规格纯度
The PIP3 Antagonist II, DM-PIT-1, also referenced under CAS 701947-53-7, controls the biological activity of PIP3.
价格
2486.58 *本价格含增值税费
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半岛bd体育手机客户端 名称:
701947-53-7
PIP3 Antagonist II, DM-PIT-1-CAS 701947-53-7-Calbiochem
N-(((2-Hydroxy-5-nitrophenyl)amino)thioxomethyl)-3,5-dimethyl-benzamide, N-((2-Hydroxy-5-nitrophenyl)carbamothioyl)-3,5-dimethylbenzamide, Akt Inhibitor XXII, PDK1 Inhibitor VI
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH domains of Akt1 (IC50≥31 ?M), ARNO, GRP1, and PKD1. Effectively blocks PIP3-dependent cellular PI3K-PDK1-Akt signaling pathway activation in U87MG (25 to 100 ?M for 3 d) and PDGF-induced Akt and GRP membrane translocation in serum-starved SUM159 cells (1 h 100 ?M pretreatment), while being inactive against PDGF-induced Btk translocation or PMA-induced PLC-δ and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles enhances its solubility (up to 1 mM) and i.v. dosing limit for more effectivein vivoadministrations (5% vs. 41% of control 4T1 tumor size in mice via 1 mg/kg micelles-formulated or 0.4 mg/kg free drug daily i.v., respectively).
A cell-permeable benzoylthiourea compound that is shown to compete against PIP3 (Cat. No. 524615) for binding PH (pleckstrin-homology) domains of Akt1 (IC50≥31 ?M using recombinant human Akt1 aa 1-123), ARNO, GRP1, and PKD1, while lacking activity against PIP3 Btk PH domain ineraction, PI-4,5-P2 (Cat. Nos. 524614, 524644, and 524646) PLC-δ PH domain binding, or PI-3,4-P2 TAPP1/2 PH domains binding, resulting in effective blockage of PIP3-dependent PI3K-PDK1-Akt signaling pathway activation in human glioblastoma U87MG cultures (25 to 100 ?M for 3 d) and (5 min 100 ng/ml) PDGF-induced Akt and GRP membrane translocation (by 85% and 70%, respectively, with 1 h 100 ?M pretreatment) in serum-starved human breast cancer SUM159 cells, while being inactive against PDGF-induced Btk translocation or (5 min 250 ng/ml) PMA-induced PLC-δ and TAPP1/2 translocations. Although DM-PIT-1 can be administered as a DMSO stock for effective culture treatments, incorporating DM-PIT-1 into PEG-PE mixed micelles is reported to enhance its solubility (up to 1 mM), and presumably delivery efficiency (57% vs. 67% U87MG viability after 24 h 50 ?M drug treatment, respectively, with or without PEG-PE encapsulation), making large dosage delivery possible for more effectivein vivoadministrations (5% vs. 41% of control 4T1 tumor size in mice after 8 daily i.v. dosages of 1 mg/kg micelles-formulated or 0.4 mg/kg free drug, respectively).

包装

25 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Miao, B., et al. 2010.Proc. Natl. Acad. Sci. USA107,20126.
Skidan, I., et al. 2009.Drug Deliv.16,45.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C16H15N3O4S
分子量 345.37
MDL编号 MFCD05129220

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 off-white
溶解性 DMSO: 25 mg/mL
运输 ambient
储存温度 2-8℃
SMILES string OC(C=CC([N+]([O-])=O)=C1)=C1NC(NC(C2=CC(C)=CC(C)=C2)=O)=S

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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