Merck
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A6730

Sigma-Aldrich

Akt1/2 kinase inhibitor

≥98% (HPLC)

All Photos(1)
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
Empirical Formula (Hill Notation):
C34H29N7O · xC2HF3O2 · yH2O
Molecular Weight:
551.64 (anhydrous free base basis)
MDL number:
MFCD08705407
PubChem Substance ID:
24891133

Quality Level

100

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

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

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This Item
124030124029SML0013
Akt1/2 kinase inhibitor ≥98% (HPLC)

Sigma-Aldrich

A6730

Akt1/2 kinase inhibitor

Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2 The Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

124030

Akt Inhibitor XIII, Isozyme-Selective, Akti2-1/2

Akt Inhibitor XII, Isozyme-Selective, Akti-2 The Akt Inhibitor XII, Isozyme-Selective, Akti-2 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

124029

Akt Inhibitor XII, Isozyme-Selective, Akti-2

Epinecidine-1 trifluoroacetate salt ≥98% (HPLC)

Sigma-Aldrich

SML0013

Epinecidine-1 trifluoroacetate salt

form

powder

form

solid

form

solid

form

powder

color

yellow

color

yellow

color

yellow

color

-

solubility

DMSO: ≥10 mg/mL

solubility

DMSO: 25 mg/mL, water: 50 mg/mL

solubility

DMSO: 25 mg/mL, water: 50 mg/mL

solubility

H2O: >2 mg/mL

originator

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

originator

-

originator

-

originator

-

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

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

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

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Sigma-Aldrich

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Sigma-Aldrich

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Akt Inhibitor XVI, AT7867

Akt Inhibitor XVIII, SC66 The Akt Inhibitor XVIII, SC66 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Millipore

124036-M

Akt Inhibitor XVIII, SC66

IL-1R Antagonist The IL-1R Antagonist, also referenced under CAS 566914-00-9, controls the biological activity of IL-1R.

Sigma-Aldrich

407616

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Sigma-Aldrich

Sigma-Aldrich

SML0749

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Sigma-Aldrich

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Perifosine

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Sigma-Aldrich

124011

Akt Inhibitor IV

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
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
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
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
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
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