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Merck

124011

Akt Inhibitor IV

≥98% (HPLC), solid

Sinónimos:

Akt Inhibitor IV

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Fórmula empírica (notación de Hill):
C31H27IN4S
Número CAS:
681281-88-9
Peso molecular:
614.54
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00570739

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Nombre del producto

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

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Contenido relacionado

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

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