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Merck

124011

Akt Inhibitor IV

≥98% (HPLC), solid

別名:

Akt Inhibitor IV

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この商品について

実験式（ヒル表記法）:
C31H27IN4S
CAS番号:
681281-88-9
分子量:
614.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00570739

主要文書

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製品名

Akt Inhibitor 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

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Akt
Product does not compete with ATP.
Reversible: yes
Target IC50: 625 nM in blocking Akt-mediated FOXO1a nuclear export; <1.25 µM in blocking Akt-mediated cell proliferation in 786-O cells

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell permeable and reversible benzimidazole compound that inhibits Akt phosphorylation/activation by targeting the ATP binding site of a kinase upstream of Akt, but downstream of PI 3-K. Shown to block Akt-mediated FOXO1a nuclear export (IC50 = 625 nM) and cell proliferation (IC50<1.25 M) in 786-O cells. Unlike phosphatidylinositol analog-based Akt inhibitors (Cat. Nos. 124005, 124008, 124009), this inhibitor does not affect PI3K. A 10 mM (1 mg/163 l) solution of Akt Inhibitor IV in DMSO is also available.
A cell-permeable and reversible benzimidazole compound that inhibits Akt phosphorylation/activation presumably by targeting the ATP binding site of a kinase upstream of Akt, but downstream of PI3-K. Shown to block Akt-mediated FOXO1a nuclear export (IC50 = 625 nM) and cell proliferation (IC50<1.25 µM) in 786-O cells. Unlike phosphatidylinositol analog-based Akt inhibitors (Cat. Nos. 124005, 124008, 124009), this inhibitor does not affect PI3-K.

Other Notes

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



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


Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

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

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

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
Roshini Fernando et al.
Journal of immunology (Baltimore, Md. : 1950), 204(7), 1724-1735 (2020-02-23)
IL-23 and IL-12, two structurally related heterodimeric cytokines sharing a common subunit, divergently promote Th cell development and expansion. Both cytokines have been implicated in the pathogenesis of thyroid-associated ophthalmopathy (TAO), an autoimmune component of Graves disease. In TAO, CD34+
Yu-Ying Chao et al.
Journal of cellular physiology (2022-10-18)
Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal cancers because of its late diagnosis and chemoresistance. Primary cilia, the cellular antennae, are observed in most human cells to maintain development and differentiation. Primary cilia are gradually lost during
Bin Li et al.
The Journal of clinical endocrinology and metabolism, 99(9), 3363-3372 (2014-05-21)
TSH provokes expression of inflammatory genes in CD34(+) fibrocytes. These cells appear to infiltrate the orbit in Graves' disease (GD), where they putatively become the CD34(+) orbital fibroblast subset (GD-OF). This may have importance in solving the pathogenesis of thyroid-associated

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Cancer Stem Cell Detection with AldeRed™ 588-A

AldeRed™ 588-A detects ALDH activity in cancer stem cells, aiding in cancer research.

関連コンテンツ

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.

Akt
Biologics 31.1

グローバルトレードアイテム番号

カタログ番号GTIN
124011-5MGCN04055977205626
124011-1MGCN04055977206357

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