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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
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00570739

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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.

SMILES string

[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

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

相关类别

Biochem/physiol Actions

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

Disclaimer

毒性：标准处理（A）

General description

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。

Other Notes

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



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


Packaging

用惰性气体包装

Preparation Note

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。

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_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
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
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
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相关内容

Biologics 31.1
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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