A6730

Akt1/2 kinase inhibitor

≥98% (HPLC)

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₃₄H₂₉N₇O · xC₂HF₃O₂ · yH₂O
• Numer CAS: 616871-83-1
• Masa cząsteczkowa: 551.64 (anhydrous free base basis)
• Numer MDL: MFCD08705407
• Kod UNSPSC: 12352200
• Identyfikator substancji w PubChem: 24891133
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Formularz: powder
• kolor: yellow
• rozpuszczalność: DMSO: ≥10 mg/mL
• inicjator: Merck & Co., Inc., Kenilworth, NJ, U.S.
• temp. przechowywania: 2-8°C
• ciąg SMILES: [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
• Klucz InChI: CRRPFKCJZALCLQ-UHFFFAOYSA-N

Opis

Zastosowanie

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.

Działania biochem./fizjol.

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.

Cechy i korzyści

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.

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable