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Merck
CN

124011

Akt抑制剂IV

≥98% (HPLC), solid

别名:

Akt抑制剂IV

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关于此项目

经验公式（希尔记法）:
C31H27IN4S
化学文摘社编号:
681281-88-9
分子量:
614.54
MDL编号:
MFCD00570739
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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产品名称

Akt抑制剂IV, The Akt Inhibitor IV, also referenced under CAS 681281-88-9, controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

质量水平

100

方案

≥98% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

颜色

yellow

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

[I-].[s]1c2c(nc1c3cc4[n](c([n+](c4cc3)c6ccccc6)C=CN(C)c5ccccc5)CC)cccc2

InChI

1S/C31H27N4S.HI/c1-3-34-28-22-23(31-32-26-16-10-11-17-29(26)36-31)18-19-27(28)35(25-14-8-5-9-15-25)30(34)20-21-33(2)24-12-6-4-7-13-24;/h4-22H,3H2,1-2H3;1H/q+1;/p-1

InChI key

NAYRELMNTQSBIN-UHFFFAOYSA-M

相关类别

一般描述

一种细胞可渗透且可逆的苯并咪唑化合物，可能通过靶向Akt上游，PI3-K下游的激酶的ATP结合位点来抑制Akt磷酸化/激活。显示可阻断786-O细胞中Akt介导的FOXO1a核输出（IC50 = 625 nM）和细胞增殖（IC50<1.25 µM）。与基于磷脂酰肌醇类似物的Akt抑制剂（目录编号124005，124008，124009）不同，该抑制剂不影响PI3-K。
一种细胞可渗透且可逆的苯并咪唑化合物，通过靶向Akt上游，PI3-K下游的激酶的ATP结合位点来抑制Akt磷酸化/激活。显示可阻断786-O细胞中Akt介导的FOXO1a核输出（IC50 = 625 nM）和细胞增殖（IC50<1.25 M）。与基于磷脂酰肌醇类似物的Akt抑制剂（目录编号124005，124008，124009）不同，该抑制剂不影响PI3K。也可获得10 mM（1 mg/163 l）Akt抑制剂IV的DMSO溶液。

生化/生理作用

主靶
Akt
产物不与ATP竞争。
可逆性：是
细胞可渗透性：具有
靶标IC50：625 nM阻断Akt介导的FOXO1a核输出；<1.25 µM阻断786-O细胞中Akt介导的细胞增殖

包装

用惰性气体包装

制备说明

在复溶后，分装并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多6个月。

其他说明

Kau, T.R., et al. 2003.Cancer Cell4, 463.



Selected Citations
Lee, J., et al. 2009.Cell Stem Cell5, 76.


法律信息

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

免责声明

毒性：标准处理（A）

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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Oleksii S Rukhlenko et al.
Nature, 609(7929), 975-985 (2022-09-15)
Understanding cell state transitions and purposefully controlling them is a longstanding challenge in biology. Here we present cell state transition assessment and regulation (cSTAR), an approach for mapping cell states, modelling transitions between them and predicting targeted interventions to convert
Mengping Zhang et al.
Journal of cellular physiology, 233(6), 4748-4758 (2017-11-18)
While overexpression of FSCN1 is reported in several cancers, the prognostic significance of FSCN1 in renal cell carcinoma (RCC) and the molecular mechanisms involved remain largely unclear. We retrospectively enrolled 194 patients with non-metastatic clear-cell RCC undergoing nephrectomy in our
Bing Xu et al.
Frontiers in neuroscience, 14, 766-766 (2020-08-28)
Poor postoperative pain (POP) control increases perioperative morbidity, prolongs hospitalization days, and causes chronic pain. However, the specific mechanism(s) underlying POP is unclear and the identification of optimal perioperative treatment remains elusive. Akt and mammalian target of rapamycin (mTOR) are
Yung-Chieh Tsai et al.
Journal of cellular biochemistry, 124(1), 89-102 (2022-10-29)
Testes control the development of male reproductive system. The testicular interstitial Leydig cells (Leydig cells) synthesize testosterone for promoting spermatogenesis and secondary sexual characteristics. Type A platelet-derived growth factor (PDGF-AA) is one of the most important growth factors in regulating
Michael Xiao et al.
eLife, 12 (2023-04-14)
Quiescent stem cells are activated in response to a mechanical or chemical injury to their tissue niche. Activated cells rapidly generate a heterogeneous progenitor population that regenerates the damaged tissues. While the transcriptional cadence that generates heterogeneity is known, the
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相关内容

Akt
Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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