Akti-1/2

製品コードS7776 バッチS777602

印刷

化学情報

Synonyms

Akt Inhibitor VIII

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₄H₂₉N₇O

分子量

551.64

CAS No.

612847-09-3

Solubility (25°C)*

体外

DMSO

22 mg/mL (39.88 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.
in vitro	In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, this compound induces cell apoptosis by dramatically increasing caspase-3 activity. ^[1] In liver cells, this chemical blocks regulation of PEPCK, G6Pase expression, and FOXO1 activity. ^[2] It also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. ^[3] In HCC827, NCI-H522, NCI-1651, and PC-9 cells, this inhibitor inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination, it causes enhanced inhibition of cell growth and apoptosis. ^[4]
in vivo	In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. ^[1]

製品説明

Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.

in vitro

In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, this compound induces cell apoptosis by dramatically increasing caspase-3 activity. ^[1]

In liver cells, this chemical blocks regulation of PEPCK, G6Pase expression, and FOXO1 activity. ^[2]

It also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. ^[3]

In HCC827, NCI-H522, NCI-1651, and PC-9 cells, this inhibitor inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination, it causes enhanced inhibition of cell growth and apoptosis. ^[4]

in vivo

In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase screen
キナーゼアッセイ	Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-³³P]-ATP, 800 cpm/pmol).
細胞アッセイ	細胞株	HCC827, NCI-H522, NCI-1651, and PC-9 cells
	濃度	~10 μM
	反応時間	96 h
	実験の流れ	The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.
動物実験	動物モデル	C57BL/6 J mice
	投薬量	50 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/15664853/
https://pubmed.ncbi.nlm.nih.gov/17563061/
https://pubmed.ncbi.nlm.nih.gov/18761726/

https://pubmed.ncbi.nlm.nih.gov/24957682/
https://pubmed.ncbi.nlm.nih.gov/34285232/

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カスタマーフィードバック

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 480(3):334-340]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 480(3):334-340.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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