MonastrolEg5 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.25%
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Chemical structure
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Cas No. | 329689-23-8 | SDF | Download SDF |
Synonyms | N/A | ||
Chemical Name | ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate | ||
Canonical SMILES | CCOC(C(C1C2=CC(O)=CC=C2)=C(N=C(S)N1)C)=O | ||
Formula | C14H16N2O3S | M.Wt | 292.35 |
Solubility | ≥29.2mg/mL in DMSO | Storage | Store at -20°C |
Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
IC50: 14 μM
Monastrol is a cell-permeable small molecule inhibitor of the mitotic kinesin, Eg5. Like other kinesins, Eg5 can drive the movement of microtubules in vitro.
In vitro: Previous study found that monastrol did not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to monastrol was also reversible rapidly. Chromosomes in monastrol-treated cells frequently had both sister kinetochores attached to microtubules extending to the center of the monoaster. Monastrol also inhibited bipolar spindle formation in Xenopus egg extracts, however, monastrol did not prevent the targeting of Eg5 to the monoastral spindles that form [1].
In vivo: Previous study investigated the rat PK and TK of LaSOM 65, a monastrol derivative. Results showed that LaSOM 65 had good bioavailability and linear PK after oral doses. LaSOM 65 distributed consistently in lung and fatty tissues. Other investigated tissues presented smaller penetration ratios. Adverse symptoms were observed only after iv administration, and regressed 3 h after dosing. No statistical differences were found for serum analysis, body weight and relative organ weight, indicating no acute toxicological effects. [2].
Clinical trial: Up to now, LaSOM 65 is still in the preclinical development stage.
References:[1] Kapoor TM,Mayer TU,Coughlin ML,Mitchison TJ. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol.2000 Sep 4;150(5):975-88.[2] Torres BG,Ucha Fde T,Pigatto MC,Azeredo FJ,Haas SE,Dallegrave E,Canto RF,Eifler-Lima VL,Dalla Costa T. Pre-clinical pharmacokinetics and acute toxicological evaluation of a monastrol derivative anticancer candidate LaSOM 65 in rats. Xenobiotica.2014 Mar;44(3):254-63.
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只有9个氨基酸,分子量1KD左右,想免疫小鼠制备单抗,有没有前辈做过这方面的东西?想了一些方法,但价值不大,请前辈们指教,不甚感激。
各位,有没有做过附件中的比对分析,用什么软件来完成的
氨基酸的结构通式:氨基酸是指一类含有羧基并在与羧基相连的碳原子下连有氨基的有机化合物。
人体所需的氨基酸约有22种,分非必需氨基酸和必需氨基酸(须从食物中供给)。另有酸性、碱性、中性、杂环分类,是根据其化学性质分类的。
1、必需氨基酸(essential amino acid): 指人体(或其它脊椎动物)不能合成或合成速度远不适应机体的需要,必需由食物蛋白供给,这些氨基酸称为必需氨基酸。共有10种其作用分别是:
(一) 赖氨酸(Lysine ):促进大脑发育,是肝及胆的组成成分,能促进脂肪代谢,调节松果腺、乳腺、黄体及卵巢,防止细胞退化;
(二) 色氨酸(Tryptophane):促进胃液及胰液的产生;
(三) 苯丙氨酸(Phenylalanine):参与消除肾及膀胱功能的损耗;
(四) 蛋氨酸(又叫甲硫氨酸)(Methionine);参与组成血红蛋白、组织与血清,有促进脾脏、胰脏及淋巴的功能;
(五) 苏氨酸(Threonine):有转变某些氨基酸达到平衡的功能;
(六) 异亮氨酸(Isoleucine ):参与胸腺、脾脏及脑下腺的调节以及代谢;脑下腺属总司令部作用于甲状腺、性腺;
(七) 亮氨酸(Leucine ):作用平衡异亮氨酸;
(八) 缬氨酸(Viline):作用于黄体、乳腺及卵巢。
(九) 组氨酸(Hlstidine):作用于代谢的调节;
(十) 精氨酸(Argnine):促进伤口愈合,精子蛋白成分。
2、非必需氨基酸(nonessential amino acid):指人(或其它脊椎动物)自己能由简单的前体合成,不需要从食物中获得的氨基酸。例如甘氨酸、丙氨酸等氨基酸。
我在看基因方面的文献。基因位点C802T的氨基酸改变H268Y是什么意思啊。求大神指教
没有这8种氨基酸就会发生由于缺乏营养所引起的疾病;氨基酸在医药上也有很大的用途,现在手术中输液都加有各种氨基酸,使患者的抵抗力增强,同时也增加营养。随着人民生活水平的提高,人们对摄入的营养物质的要求越来越高,尤其是幼儿、青少年的健康成长,疾病患者的康复,都迫切需要高质量的营养物质,所以有效开发氨基酸食品是很有必要的。
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