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BrBzGCp2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BrBzGCp2图片
CAS NO:166038-00-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
BrBzGCp2是乙二醛酶1(GLO1)的抑制剂,其GC50为4.23μM(HL-60细胞)。BrBzGCp2具有抗肿瘤和神经保护活性。
Cas No.166038-00-2
别名S-p-Bromobenzylglutathione cyclopentyl diester
Canonical SMILESO=C(NCC(OC1CCCC1)=O)[C@@H](NC(CC[C@H](N)C(OC2CCCC2)=O)=O)CSCC(C=C3)=CC=C3Br
分子式C27H38BrN3O6S
分子量612.58
溶解度DMSO: 250 mg/mL (408.11 mM)
储存条件-20℃, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity[1][2].

GLO1 inhibition by BrBzGCp2 increases center time in the OF test, without changing distance traveled. GLO1 inhibition increases MG (methylglyoxal) concentration, thus reducing anxiety-like behavior[2]. BrBzGCp2 pre-treatment decreases seizure duration[3].BrBzGCp2 injection alleviates the level of anxiety in mice, and mice with less anxiety and fear were more likely to explore the unknown area, implying that inhibition of GLO1 activity mitigated anxiety levels[4].BrBzGCp2 treatment restores the VPA-induced inhibition effect on GABAA receptor activation[4].BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice[5]. Animal Model: Male CD-1 mice[2].

[1]. P J Thornalley, et al. Antitumor activity of S-(p-bromobenzyl)glutathione diesters in vitro: a structure-activity study. J Med Chem. 1996 Aug 16;39(17):3409-11. [2]. Margaret G Distler, et al. Glyoxalase 1 increases anxiety by reducing GABAA receptor agonist methylglyoxal. J Clin Invest. 2012 Jun;122(6):2306-15. [3]. Katherine M. J. McMurray, et al. GLO1 inhibitors for neuropsychiatric and anti-epileptic drug development. Biochem Soc Trans. 2014 Apr;42(2):461-7. [4]. Margaret G Distler, et al. Glyoxalase 1 and its substrate methylglyoxal are novel regulators of seizure susceptibility. Epilepsia. 2013 Apr;54(4):649-57. [5]. Tao Xu, et al. GW29-e0826 ARC Regulates Programmed Necrosis and Myocardial Ischemia/Reperfusion Injury through Preventing the Opening of mPTP. J Am Coll Cardiol. 2018 Oct, 72 (16_Supplement) C27.