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Merck
CN
所有图片(1)

文件

A6730

Sigma-Aldrich

Akt1/2激酶抑制剂

≥98% (HPLC)

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所有图片(1)
别名:
1,3-二氢-1-（1-（（4-（6-苯基-1H-咪唑[4,5-g）喹喔啉-7-基）苯基）甲基）-4-哌啶基）-2H-苯并咪唑-2-酮 三氟乙酸盐 水合物, Akti-1/2 三氟乙酸盐 水合物, Akt抑制剂八 三氟乙酸盐 水合物
经验公式（希尔记法）:
C34H29N7O · xC2HF3O2 · yH2O
CAS号:
616871-83-1
分子量:
551.64 (anhydrous free base basis)
MDL编号:
MFCD08705407
UNSPSC代码:
12352200
PubChem化学物质编号:
24891133
NACRES:
NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

颜色

yellow

溶解性

DMSO: ≥10 mg/mL

创始人

Merck & Co., Inc., Kenilworth, NJ, U.S.

储存温度

2-8°C

SMILES字符串

[H]O[H].OC(=O)C(F)(F)F.O=C1Nc2ccccc2N1C3CCN(CC3)Cc4ccc(cc4)-c5nc6cc7nc[nH]c7cc6nc5-c8ccccc8

InChI

1S/C34H29N7O.C2HF3O2.H2O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33;3-2(4,5)1(6)7;/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42);(H,6,7);1H2

InChI key

CRRPFKCJZALCLQ-UHFFFAOYSA-N

应用

Akt在细胞增殖、凋亡、血管生成和糖尿病的信号转导途径中发挥作用。Akt1和Akt2双激酶抑制剂能够使肿瘤细胞对某些凋亡刺激敏感，并抑制体内Akt磷酸化。造血细胞中Akt1激酶的活性及其受细胞体内外信号因子的调节表明，AKT1的激活涉及激酶从胞质溶胶到膜的胞内易位。

生化/生理作用

同工酶选择性Akt1/2激酶抑制剂。在体外激酶试验中，Akt1/2激酶抑制剂显示IC50 = 58 nM、210 nM和2.12 mM，分别针对Akt1、Akt2和Akt3，抑制作用似乎是多重同源（酸碱度）结构域依赖性的，Akt1/2激酶抑制剂对酸碱度结构域缺失的Akts或其他密切相关的AGC家族激酶、PKA、PKC和SGK没有抑制作用，即使浓度高达50 & # 956；M.

特点和优势

该化合物由Merck & Co., Inc.（美国新泽西州Kenilworth）开发。想要浏览其他由制药公司开发的化合物以及已批准药物/候选药物清单， 请单击此处。
这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

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访问文档库

Zhijian Zhao et al.
Bioorganic & medicinal chemistry letters, 15(4), 905-909 (2005-02-03)
This letter describes the discovery of a novel series of dual Akt1/Akt2 kinase inhibitors, based on a 2,3,5-trisubstituted pyridine scaffold. Compounds from this series, which contain a 5-tetrazolyl moiety, exhibit more potent inhibition of Akt2 than Akt1.
Brad Larson et al.
Assay and drug development technologies, 7(6), 573-584 (2010-01-12)
Kinases continue to be one of the most important targets in today's drug discovery efforts. Following the identification of lead compounds through screening efforts, it is important to profile these leads against other kinases within that family, as well as
X Zhang et al.
Leukemia research, 21(9), 849-856 (1997-12-11)
AKT1 is the human homolog of the v-akt oncogene. AKT1 has two distinct protein domains, one serine/threonine kinase domain and one pleckstrin homology (PH) domain. We studied the expression and activity of AKT1 in hematopoietic cell lines. The expression of
Z Lu et al.
Cell death and differentiation, 21(8), 1275-1289 (2014-04-29)
The process of autophagy has been described in detail at the molecular level in normal cells, but less is known of its regulation in cancer cells. Aplasia Ras homolog member I (ARHI; DIRAS3) is an imprinted tumor suppressor gene that
Jenny Sandström et al.
Archives of toxicology, 93(6), 1649-1664 (2019-04-18)
Brain susceptibility to a neurotoxic insult may be increased in a compromised health status, such as metabolic syndrome. Both metabolic syndrome and exposure to trimethyltin (TMT) are known to promote neurodegeneration. In combination the two factors may elicit additive or
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