A6730

Akt1/2 kinase inhibitor

Name: Akt1/2 kinase inhibitor
Brand: SIGMA

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

Synonym(s):

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

Empirical Formula (Hill Notation):

C₃₄H₂₉N₇O · xC₂HF₃O₂ · yH₂O

CAS Number:

616871-83-1

Molecular Weight:

551.64 (anhydrous free base basis)

UNSPSC Code:

12352200

PubChem Substance ID:

24891133

NACRES:

NA.77

MDL number:

MFCD08705407

Key Documents

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Product Name

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

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Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

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1 of 4

This Item	124018	124030	124029
Sigma-Aldrich A6730 Akt1/2 kinase inhibitor	Sigma-Aldrich 124018 Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2	Sigma-Aldrich 124030 Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2	Sigma-Aldrich 124029 Akt Inhibitor XII, Isozyme-Selective, Akti-2
form powder	form solid	form solid	form solid
assay ≥98% (HPLC)	assay ≥95% (HPLC)	assay ≥97% (mixture of regioisomers, HPLC)	assay ≥97% (mixture of regioisomers, HPLC)
Quality Level 100	Quality Level 200	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: ≥10 mg/mL	solubility DMSO: 5 mg/mL	solubility DMSO: 25 mg/mL, water: 50 mg/mL	solubility DMSO: 25 mg/mL, water: 50 mg/mL
originator Merck & Co., Inc., Kenilworth, NJ, U.S.	originator -	originator -	originator -

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number

0000223096

0000190470

0000143305

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ARHI (DIRAS3) induces autophagy in ovarian cancer cells by downregulating the epidermal growth factor receptor, inhibiting PI3K and Ras/MAP signaling and activating the FOXo3a-mediated induction of Rab7.

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

Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.

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.

A Simple and robust automated kinase profiling platform using luminescent ADP accumulation technology.

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

Growth factor stimulation of hematopoietic cells leads to membrane translocation of AKT1 protein kinase.

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

In vitro models to study insulin and glucocorticoids modulation of trimethyltin (TMT)-induced neuroinflammation and neurodegeneration, and in vivo validation in db/db mice.

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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