Akti-1/2

製品コードS7776 バッチS777602

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
* <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.

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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, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. ^[1] In liver cells, Akti-1/2 blocks insulin regulation of PEPCK, G6Pase expression, and FOXO1 activity. ^[2] Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. ^[3] In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination with gefitinib, Akti-1/2 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, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. ^[1]

In liver cells, Akti-1/2 blocks insulin regulation of PEPCK, G6Pase expression, and FOXO1 activity. ^[2]

Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. ^[3]

In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination with gefitinib, Akti-1/2 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

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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.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Combined inhibition of HER2 and VEGFR synergistically improves therapeutic efficacy via PI3K-AKT pathway in advanced ovarian cancer [ J Exp Clin Cancer Res, 2024, 43(1):56]	PubMed: 38403634
P. gingivalis Infection Upregulates PD-L1 Expression on Dendritic Cells, Suppresses CD8+ T-cell Responses, and Aggravates Oral Cancer [ Cancer Immunol Res, 2023, 11(3):290-305]	PubMed: 36633576
P. gingivalis Infection Upregulates PD-L1 Expression on Dendritic Cells, Suppresses CD8+ T-cell Responses, and Aggravates Oral Cancer [ Cancer Immunol Res, 2023, 11(3):290-305]	PubMed: 36633576
Colorectal Cancer Patient-Derived 2D and 3D Models Efficiently Recapitulate Inter- and Intratumoral Heterogeneity [ Adv Sci (Weinh), 2022, e2201539]	PubMed: 35652270
PSMG2-controlled proteasome-autophagy balance mediates the tolerance for MEK-targeted therapy in triple-negative breast cancer [ Cell Rep Med, 2022, 3(9):100741]	PubMed: 36099919
A hotspot mutation targeting the R-RAS2 GTPase acts as a potent oncogenic driver in a wide spectrum of tumors [ Cell Rep, 2022, 38(11):110522]	PubMed: 35294890
Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry [ Elife, 2022, 11e77696]	PubMed: 35439114
NHERF4 hijacks Mas-mediated PLC/AKT signaling to suppress the invasive potential of clear cell renal cell carcinoma cells [ Cancer Lett, 2021, 519:130-140]	PubMed: 34216689
The Protective Role of TLR2 Mediates Impaired Autophagic Flux by Activating the mTOR Pathway During Neospora caninum Infection in Mice [ Front Cell Infect Microbiol, 2021, 11:788340]	PubMed: 34900761
TANK-binding kinase 1 inhibitor GSK8612 enhances daunorubicin sensitivity in acute myeloid leukemia cells via the AKT-CDK2 pathway [ Am J Transl Res, 2021, 13(12):13640-13653]	PubMed: 35035703

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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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