AKT inhibitor VIII

Modify Date: 2024-01-02 18:02:38

AKT inhibitor VIII structure	Common Name	AKT inhibitor VIII
	CAS Number	612847-09-3	Molecular Weight	551.640
	Density	1.4±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₃₄H₂₉N₇O	Melting Point	242-245ºC (dec.)
	MSDS	N/A	Flash Point	N/A

Use of AKT inhibitor VIII

AKT inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

Name	3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
Synonym	More Synonyms

Description	AKT inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> Akt Research Areas >> Cancer
Target	Akt1:58 nM (IC50) Akt2:210 nM (IC50) Akt3:2119 nM (IC50)
In Vitro	When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin[1]. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions[2]. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1)[3].
In Vivo	Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation[1].
Cell Assay	PSC are plated onto Matrigel coated 96-well plates at densities between 1×103-3×105 cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm.
References	[1]. Lindsley, et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg. Med. Chem. Lett. (2005), 15(3), 761-764. [2]. Zhong Z, et al. Furanodiene, a Natural Product, Inhibits Breast Cancer Growth Both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. Epub 2012 Aug 2. [3]. Leonardo Romorini, et al. AKT/GSK3β signaling pathway is critically involved in human pluripotent stem cell survival. Sci Rep. 2016; 6: 35660

Density	1.4±0.1 g/cm3
Melting Point	242-245ºC (dec.)
Molecular Formula	C₃₄H₂₉N₇O
Molecular Weight	551.640
Exact Mass	551.243347
PSA	95.49000
LogP	5.10
Index of Refraction	1.734

2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-

Akti-1/2

1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one

1-{1-[4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one

Akt inhibitor VIII

1-{1-[4-(6-Phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)benzyl]-4-piperidinyl}-1,3-dihydro-2H-benzimidazol-2-one

imidazoquinoxaline 16h

Akt Inhibitor VIII,Isozyme-Selective,Akti-1/2

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: AKT inhibitor VIII
Price: Click To Check
Purity: 98.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: AKT inhibitor VIII
Price: ￥6326.0/100mg ￥976.0/5mg ￥2536.0/25mg ￥4386.0/50mg
Purity: 98.0%
Delivery: 2 Day
Contact: Liu jia
Email: 2130147988@qq.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: Akt Inhibitor VIII
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: Akt Inhibitor VIII
Price: $400.0/100mg $800.0/250mg $1600.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 1-(1-(4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)BENZYL)PIPERIDIN-4-YL)-1H-BENZO[D]IMIDAZOL-2(3H)-ONE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Delivery: Inquiry
Contact: Ms Wang
Email: enquiry@dycnchem.com

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Price: $146/10mM*1mLinDMSO

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AKT inhibitor VIII

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