AKT Inhibitors
본문
AKT Inhibitors
Product Name: Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
A cell-permeable quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology
(PH) domain-dependent. It does not exhibit any 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. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.
Details
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Chemical Formula:
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C34H29N7O
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CAS No.:
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612847-09-3
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Molecular weight:
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551.6
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Purity:
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98% by HPLC
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Appearance:
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Light yellow solid
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Chemical name:
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1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4- piperidinyl)-2H-benzimidazol-2-one
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Solubility:
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DMSO (5mg/mL)
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Storage:
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Protect from light. Packaged under inert gas
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References
A cell-permeable, reversible, and selective inhibitor of the phosphorylation of Akt and its in vitro kinase activity (complete
inhibition < 5 µM) with minimal effect on PI 3-K, PDK1, or SGK1. Shown to suppress growth of Rh (rhabdomyosarcoma) cell
lines (IC50 = 2-5 μM), inhibit IGF-I-stimulated nuclear translocation of Akt, and prevent phosphorylation of the downstream
targets, mTOR, p70S6 kinase, and S6 ribosomal protein. Unlike Akti1/2 (Cat # CD0223), the mode of inhibition is not PH
domain-dependent. Also shown to induce neuronal autophagy in an Akt- and mTOR-independent manner and enhances the
clearance of misfolded protein.
Details
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Chemical Formula:
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C20H25CIN2O∙HCI
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CAS No.:
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925681-41-0
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Molecular weight:
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381.4
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Purity:
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98% by HPLC
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Appearance:
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White solid
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Chemical name:
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10-(4′-(N-diethylamino)butyl)-2-chlorophenoxazine hydrochloride
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Solubility:
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DMSO (60 mg/mL), water (1 mg/mL)
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Storage:
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Protect from light. Packaged under inert gas
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References
Ordering informations
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Catalog No.
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Product Name
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Size
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CD0223
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AKT inhibitor VIII
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1mg, 5mg, 10mg & 25mg
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CD0225
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AKT inhibitor X
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1mg, 5mg, 10mg & 25mg
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