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Merck

A6730

Akt1/2 kinase inhibitor

≥98% (HPLC), Akt1/2 kinase inhibitor, powder

Sinónimos:

1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one trifluoroacetate salt hydrate, Akt Inhibitor VIII trifluoroacetate salt hydrate, Akti-1/2 trifluoroacetate salt hydrate

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About This Item

Fórmula empírica (notación de Hill):
C34H29N7O · xC2HF3O2 · yH2O
Número CAS:
616871-83-1
Peso molecular:
551.64 (anhydrous free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
24891133
NACRES:
NA.77
MDL number:
MFCD08705407

Nombre del producto

Akt1/2 kinase inhibitor, ≥98% (HPLC)

SMILES string

[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

assay

≥98% (HPLC)

form

powder

color

yellow

solubility

DMSO: ≥10 mg/mL

originator

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

storage temp.

2-8°C

Quality Level

100

Categorías relacionadas

Application

Akt plays a role in signal transduction pathways of cell proliferation, apoptosis, angiogenesis, and diabetes. Akt1 and Akt2 dual kinase inhibitors are capable of sensitizing tumor cells to certain apoptotic stimuli, and inhibit Akt phosphorylation in vivo. Akt1 kinase activity and its regulation by extracellular signaling factors in vivo in hematopoietic cells suggests the activation of AKT1 involves intracellular translocation of the kinase from cytosol to membrane.

Biochem/physiol Actions

Akt1/2 kinase inhibitor; isozyme selective with preference toward Akt1.
Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000223096
0000223096
0000190470
0000190470
0000142885

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Visite la Librería de documentos

Subhash Ajmani et al.
Journal of molecular graphics & modelling, 28(7), 683-694 (2010-02-16)
Protein kinase B (PKB, also known as Akt) belongs to the AGC subfamily of the protein kinase superfamily. Akt1 has been reported as a central player in regulation of metabolism, cell survival, motility, transcription and cell-cycle progression, among the signalling
Denise Treue et al.
International journal of cancer, 144(3), 545-557 (2018-09-06)
Cancer precision medicine largely relies on knowledge about genetic aberrations in tumors and next-generation-sequencing studies have shown a high mutational complexity in many cancers. Although a large number of the observed mutations is believed to be not causally linked with
Shaomin Peng et al.
Experimental eye research, 151, 179-189 (2016-09-07)
Mutations of claudin-19 cause severe ocular deficits that are not easily reconciled with its role in regulating the outer blood retinal barrier. ARPE-19 is a widely used culture model of the retinal pigment epithelium (RPE). ARPE-19 is unique among epithelial
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
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