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SC 79 目录号 GC11645

Akt activator

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50mg
¥1,806.00
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10mg
¥620.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

HsSultan or NB4 cells (2.5×105) are plated in a 24-well plate in 500 μL of phenol red-free RPMI medium supplemented with 10% FBS. After incubation for 24 hours, each compound (8 µg/mL) is added and cultured for overnight (16-20 h). Fifty μLs of MTT solution (5 mg/mL in PBS) are added to each well. Following 2 hrs incubation, the purple formazan crystals are dissolved by directly adding in 500 μL of isopropanol with 0.1mol/LHCl to each well. After clearing the cell debris by centrifugation, the absorbance is measured at a wavelength of 570 nm.

Animal experiment:

The permanent focal cerebral ischemia is induced by middle cerebral artery occlusion (MCAO) essentially. Briefly, mice (C57 Black/6) weighing 17-25 g are anesthetized with 4% isoflurane/66% N2O/30% O2 and maintained with 1.5% isoflurane. Permanent focal ischemia is achieved as follows: a 2-mm hole is drilled at a site superior and lateral to the left foramen ovale to expose the left middle cerebral artery. The proximal portion of the left middle cerebral artery (MCA) is permanently occluded over a 1-mm segment distal to the origin of the lenticulostriate branches through the use of a bipolar coagulator. SC79 is injected intraperitoneally (0.04 mg/g mouse body weight) 5 min before permanent MCAO. In another experiment, extra SC79 is injected (0.04 mg/g mouse body weight, once per hour for 6 hours).

References:

[1]. Jo H, et al. Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death. Proc Natl Acad Sci U S A. 2012 Jun 26;109(26):10581-10586.
[2]. So EY, et al. BRAT1 deficiency causes increased glucose metabolism and mitochondrial malfunction. BMC Cancer. 2014 Jul 29;14:548

Chemical Properties

Cas No. 305834-79-1 SDF
别名 N/A
化学名 ethyl 2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
Canonical SMILES CCOC(C(C(C(C(OCC)=O)=C1N)C2=C(O1)C=CC(Cl)=C2)C#N)=O
分子式 C17H17ClN2O5 分子量 364.78
溶解度 ≥ 36.5mg/mL in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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SC 79 is an activator of Akt. Akt/PKB with anti-apoptotic activity (a serine/threonine protein kinase) is one of the major downstream targets of PtdIns P3 signaling pathway.

In vitro: SC79 was identified by a cell-based high-throughput chemical genetic screening, and inhibits Akt membrane translocation. However, Akt was paradoxically activated by SC79in the cytosol, specifically binding to the PH domain of Akt. The conformation of SC79-bound Akt is favorable for phosphorylation by upstream protein kinases. In a mouse model and a hippocampal neuronal culture system for ischemic stroke, the result of augmented neuronal survival is attained, based on the cytosolic activation of Akt by SC79, which is sufficient to recapitulate the primary cellular function of Akt signaling. Thus, SC79, a unique specific Akt activator, may be applied to enhance Akt activity in various physiological and pathological conditions.

In vivo: In aqueous environment, SC79 is relatively unstable. Intriguingly, however, the sustained level of phosphorylated Akt was observed both in cell culture and in vivo after the removal of SC79, indicating that SC79 may act irreversibly. The chemical moieties of SC79 (i.e., nitrile group) could be modified and/or reacts with amino acids. Nevertheless, SC79, a relatively safe drug, was revealed by following fact. Assignment of SC79 treatment much high dose (0.4 mg/g of body weight) did not accelerate any detectable changes in body weight (survival rate, appearance, and behavior) in mice. Achievement of neuronal protective effect by i.p. injection suggests that SC79 also has a good penetration of blood–brain barrier. SC79 can be applied as a chemical platform to develop novel drugs for neurological and other complications

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Jo H, Mondal S, Tan D, Nagata E, Takizawa S, Sharma AK, Hou Q, Shanmugasundaram K, Prasad A, Tung JK, Tejeda AO, Man H, Rigby AC, Luo HR.  Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death. Proc Natl Acad Sci U S A. 2012 Jun 26; 109 (26):10581-6.