AKT inhibitor VIII (Synonyms: AKTi-1/2)

目录号: HY-10355 纯度: 98.18%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

AKT inhibitor VIII (AKTi-1/2) 是一种细胞渗透的喹喔啉化合物，能够有效的，选择性的，可逆的抑制 Akt1，Akt2 和 Akt3 的活性，IC₅₀ 值分别为 58 nM，210 nM 和 2119 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

AKT inhibitor VIII Chemical Structure

CAS No. : 612847-09-3

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1456	In-stock
1 mg	￥545	In-stock
5 mg	￥1200	In-stock
10 mg	￥2000	In-stock
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of AKT inhibitor VIII:

PF-AKT400 In-stock

MCE 顾客使用本产品发表的 44 篇科研文献

: AKT inhibitor VIII purchased from MCE. Usage Cited in: Nutrients. 2018 Sep 23;10(10). pii: E1366. [Abstract]; Competition tests of SC79, PHT-427, AT7867, and AKT inhibitor VIII with the CGA probe against enriched AKT by CGA-modified functionalized MMs. Bands of AKT are detected by Western blot.

: AKT inhibitor VIII purchased from MCE. Usage Cited in: Cell Death Dis. 2017 May 25;8(5):e2817. [Abstract]; Injury-induced follicular activation is blocked by the mTOR inhibitor rapamycin. Mice are treated with specific inhibitors of the signaling pathways 12 h before surgery and another injection is given just after the surgery. Ovaries are collected at 6 h or 3 weeks after the surgery. C, control ovaries; S, surgically treated ovaries; Rapamycin, mTORC1 inhibitor; Akt VIII, Akt inhibitor; U0126, MAPK inhibitor. Specific inhibition of corresponding signaling pathways by inhibitors. Ovaries are collec

AKT inhibitor VIII 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Akt 亚型特异性产品:

查看所有亚型

Akt Akt1 Akt2 Akt3

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.

IC₅₀ & Target^[1]

Akt1

58 nM (IC₅₀)

Akt2

210 nM (IC₅₀)

Akt3

2119 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
184B5	GI₅₀	25.76 μM Compound: 8	Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay	[PMID: 18691894]
184B5	GI₅₀	50.58 μM Compound: 8	Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay	[PMID: 18691894]
184B5	GI₅₀	60.6 μM Compound: 8	Cytotoxicity against human 184B5 cells by SRB assay Cytotoxicity against human 184B5 cells by SRB assay	[PMID: 18691894]
Hep 3B2	IC₅₀	3.5 μM Compound: 14	Anticancer activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay Anticancer activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay	[PMID: 33873056]
HL-60	IC₅₀	5.5 μM Compound: A6730	Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay	[PMID: 26945110]
Huh-7	IC₅₀	4 μM Compound: 14	Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay	[PMID: 33873056]
Jurkat	IC₅₀	3.5 μM Compound: A6730	Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay	[PMID: 26945110]
K562	IC₅₀	17 μM Compound: A6730	Antiproliferative activity against human K562 cells measured after 3 days by MTS assay Antiproliferative activity against human K562 cells measured after 3 days by MTS assay	[PMID: 26945110]
MCF7	GI₅₀	0.05 μM Compound: 8	Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MCF7	GI₅₀	0.41 μM Compound: 8	Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MCF7	GI₅₀	0.92 μM Compound: 8	Cytotoxicity against human MCF7 cells by SRB assay Cytotoxicity against human MCF7 cells by SRB assay	[PMID: 18691894]
MDA-MB-231	GI₅₀	2.95 μM Compound: 8	Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-231	GI₅₀	4.55 μM Compound: 8	Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-231	GI₅₀	5.31 μM Compound: 8	Cytotoxicity against human MDA-MB-231 cells by SRB assay Cytotoxicity against human MDA-MB-231 cells by SRB assay	[PMID: 18691894]
MDA-MB-468	GI₅₀	0.85 μM Compound: 8	Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-468	GI₅₀	2.66 μM Compound: 8	Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-468	GI₅₀	6.3 μM Compound: 8	Cytotoxicity against human MDA-MB-468 cells by SRB assay Cytotoxicity against human MDA-MB-468 cells by SRB assay	[PMID: 18691894]
PBMC	IC₅₀	> 50 μM Compound: A6730	Cytotoxicity against PHA induced human PBMC after 3 days by MTS assay Cytotoxicity against PHA induced human PBMC after 3 days by MTS assay	[PMID: 26945110]
U-937	IC₅₀	8 μM Compound: A6730	Antiproliferative activity against human U937 cells measured after 3 days by MTS assay Antiproliferative activity against human U937 cells measured after 3 days by MTS assay	[PMID: 26945110]

体外研究
(In Vitro)

当 LnCaP 细胞用 AKT inhibitor VIII 预处理，然后用 TRAIL 孵育时，可以观察到 caspase-3 活性急剧增加（相对于对照或单独的 TRAIL 增加 6-10 倍）。AKT inhibitor VIII 对肿瘤细胞系的这种致敏作用并不局限于 LnCaP 细胞，因为在 HT29、MCF7 和 A2780 细胞等细胞中也观察到了类似的凋亡诱导，其中使用化学增敏剂如喜树碱、赫赛汀和阿霉素^[1]。
AKT inhibitor VIII 预处理可增强呋喃二烯诱导的 p-Akt 和 Akt 表达下降。此外，AKT inhibitor VIII 预处理可增强呋喃二烯诱导的 PARP 裂解。 AKT inhibitor VIII 对裂解的 PARP 表达没有影响，但会降低 p-Akt 和 Akt 表达^[2]。
AKT inhibitor VIII 会降低细胞活力，并增加 hESC 系 WA01 (H1) 和 WA09 (H9) 以及我们实验室生成的 hiPSC 细胞系 (FN2.1) 中的磷脂酰丝氨酸 (PS) 易位至质膜外层、DNA 碎片化、Caspase-9 裂解、Caspase-3 活化和 PARP 蛋白水解^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

给小鼠注射 AKT inhibitor VIII（50 mpk，3 次剂量，腹腔注射，每 90 分钟一次）以达到 1.5-2.0 μM 的血浆浓度，然后给动物尾静脉注射 IGF 以刺激 Akt 磷酸化。通过 IP Western，小鼠肺中基础和 IGF 刺激的 Akt1 和 Akt2 磷酸化均受到抑制，对 Akt3 磷酸化没有影响^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

551.64

Formula

C₃₄H₂₉N₇O

CAS 号

612847-09-3

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 20 mg/mL (36.26 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8128 mL	9.0639 mL	18.1278 mL
5 mM	0.3626 mL	1.8128 mL	3.6256 mL
10 mM	0.1813 mL	0.9064 mL	1.8128 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (3.63 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (3.63 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.97%

选择批次：

Data Sheet (659 KB) SDS (597 KB)

COA (291 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lindsley, et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg. Med. Chem. Lett. (2005), 15(3), 761-764. [Content Brief]

[2]. Zhong Z, et al. Furanodiene, a Natural Product, Inhibits Breast Cancer Growth Both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. Epub 2012 Aug 2. [Content Brief]

[3]. Leonardo Romorini, et al. AKT/GSK3β signaling pathway is critically involved in human pluripotent stem cell survival. Sci Rep. 2016; 6: 35660

Cell Assay ^[3]	PSC are plated onto Matrigel coated 96-well plates at densities between 1×10³-3×10⁵ cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lindsley, et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg. Med. Chem. Lett. (2005), 15(3), 761-764. [Content Brief] [2]. Zhong Z, et al. Furanodiene, a Natural Product, Inhibits Breast Cancer Growth Both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. Epub 2012 Aug 2. [Content Brief] [3]. Leonardo Romorini, et al. AKT/GSK3β signaling pathway is critically involved in human pluripotent stem cell survival. Sci Rep. 2016; 6: 35660

Cell Assay
^[3]

PSC are plated onto Matrigel coated 96-well plates at densities between 1×10³-3×10⁵ cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Lindsley, et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg. Med. Chem. Lett. (2005), 15(3), 761-764. [Content Brief]

[2]. Zhong Z, et al. Furanodiene, a Natural Product, Inhibits Breast Cancer Growth Both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. Epub 2012 Aug 2. [Content Brief]

[3]. Leonardo Romorini, et al. AKT/GSK3β signaling pathway is critically involved in human pluripotent stem cell survival. Sci Rep. 2016; 6: 35660

AKT inhibitor VIII 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8128 mL	9.0639 mL	18.1278 mL	45.3194 mL
	5 mM	0.3626 mL	1.8128 mL	3.6256 mL	9.0639 mL
	10 mM	0.1813 mL	0.9064 mL	1.8128 mL	4.5319 mL
	15 mM	0.1209 mL	0.6043 mL	1.2085 mL	3.0213 mL
	20 mM	0.0906 mL	0.4532 mL	0.9064 mL	2.2660 mL
	25 mM	0.0725 mL	0.3626 mL	0.7251 mL	1.8128 mL
	30 mM	0.0604 mL	0.3021 mL	0.6043 mL	1.5106 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AKT inhibitor VIII612847-09-3AKTi-1/2AktApoptosisPKBProtein kinase BInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

AKT inhibitor VIII (Synonyms: AKTi-1/2)

Customer Review

Other Forms of AKT inhibitor VIII:

MCE 顾客使用本产品发表的 44 篇科研文献

AKT inhibitor VIII 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Akt 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

AKT inhibitor VIII 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

AKT inhibitor VIII (Synonyms: AKTi-1/2)

Customer Review

Other Forms of AKT inhibitor VIII:

AKT inhibitor VIII 相关抗体

MCE 顾客使用本产品发表的 44 篇科研文献

AKT inhibitor VIII 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Akt 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

AKT inhibitor VIII 相关抗体:

摩尔计算器

稀释计算器

AKT inhibitor VIII 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z