Glyoxalase I inhibitor
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Glyoxalase I 抑制剂即3(Et)2,是一种有效的glyoxalase I抑制剂。由于S-(N-芳基-N-羟基氨基)谷胱甘肽衍生物能强烈抑制甲基乙二醛解毒酶glyoxalase I,现已被提出可能作为一种抗癌药物。
体外试验:作为一种肿瘤选择性抗癌试剂,评估Glyoxalase I抑制剂对培养的B16黑色素瘤、L1210小鼠白血病和非增殖性小鼠脾淋巴细胞的作用。体外试验表明,与正常小鼠脾淋巴细胞相比,Glyoxalase I抑制剂的二乙酯前药对L1210细胞有显著的肿瘤选择性细胞毒性[1]。
体内试验:小规模的功效研究表明,3b(Et)2可有效抑制含小鼠B16黑色素瘤的血浆酯酶缺陷型小鼠以及含雄激素非依赖性人前列腺PC-3肿瘤或人类结肠HT-29肿瘤的酯酶缺陷型无胸腺裸鼠中肿瘤的生长[2]。
临床试验:没有可用的临床数据[1]。
参考文献:
[1] Kavarana MJ, Kovaleva EG, Creighton DJ, Wollman MB, Eiseman JL. Mechanism-based competitive inhibitors of glyoxalase I: intracellular delivery, in vitro antitumor activities, and stabilities in human serum and mouse serum. J Med Chem. 1999;42(2):221-8.
[2] Creighton DJ, Zheng ZB, Holewinski R, Hamilton DS, Eiseman JL. Glyoxalase I inhibitors in cancer chemotherapy. Biochem Soc Trans. 2003;31(Pt 6):1378-82.
Storage | Store at -20°C |
M.Wt | 613.91 |
Cas No. | 221174-33-0 |
Formula | C21H30BrClN4O8S |
Solubility | Soluble in DMSO |
Chemical Name | ethyl (2S)-2-amino-5-[[(2R)-3-[(4-bromophenyl)-hydroxycarbamoyl]sulfanyl-1-[(2-ethoxy-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate hydrochloride |
SDF | Download SDF |
Canonical SMILES | CCOC(=O)CNC(=O)C(CSC(=O)N(C1=CC=C(C=C1)Br)O)NC(=O)CCC(C(=O)OCC)N.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | Glyoxalase I inhibitor 是一种有效的乙二醛酶I(glyoxalase I)抑制剂。 | |||||
靶点 | glyoxalase I | |||||
IC50 |