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当前位置: 首页> 产品中心> 信号转导研究相关 > Ca/cAMP/脂质信号通路 > Calyculin A 花萼海绵体诱癌素A
Calyculin A 花萼海绵体诱癌素A
目录号 MZ2504-100UG 售价 4862.00元
规格 100 µg 运输温度 冰袋
其他名称 N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy- 1-meth 保存温度 -20ºC避光干燥保存
CAS号 101932-71-2 有效期 2年
应用 蛋白磷酸酶1(PP1)和蛋白磷酸酶2A(PP2A)抑制剂 订购数量
产品简介:

Calyculin A 花萼海绵体诱癌素A


产品标签

Calyculin A;Okadaic acid 冈田软海绵酸;Protein phosphatase 1 (PP1);Protein phosphatase 2A (PP2A) ;Tumor Promoter 肿瘤促进剂;CAS NO:101932-71-2;


产品信息

产品名称

产品编号

CAS NO.

规格             

价格(元)   

Calyculin A 花萼海绵体诱癌素A    

MZ2504-25UG        

101932-71-2   

25 µg

2060

Calyculin A 花萼海绵体诱癌素A

MZ2504-50UG

101932-71-2

50 µg

3262

Calyculin A 花萼海绵体诱癌素A

MZ2504-100UG

101932-71-2

100 µg

4862


产品描述

花萼海绵体诱癌素A(Calyculin A,CAS NO:101932-71-2)最初是从海绵Disodermia calyx中分离到的一种海洋毒素,是一种具细胞渗透性、有效和选择性的蛋白磷酸酶1(PP1,IC50=0.3-0.7 nM)和蛋白磷酸酶2A(PP2A,IC50=0.5-1.0 nM)抑制剂。对PP2B和PP2C的选择性>10,000,000倍。对酸性或碱性磷酸酶或磷酸-酪氨酸蛋白磷酸酶无抑制。Calyculin A抑制平滑肌肌球蛋白B内源性磷酸酶的活性,诱导肌肉纤维收缩,并伴随细胞质游离Ca2+水平提高。花萼海绵体诱癌素A还是一种非佛波类的肿瘤促进剂。与小鼠皮肤上的蛋白磷酸酶结合,诱导鸟氨酸脱羧酶(ODC)活性,进而促进肿瘤生长。


产品特性

1) CAS NO:101932-71-2

2) 化学名:N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy- 1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-oxazoly]butyl]-4-deoxy-4-(dimethylamino)-5-O-methyl-L-ribonamide

3) 分子式:C50H81N4O15P

4) 分子量:1009.17

5) 纯度:≥98%

6) 外观:透明薄膜或白色结晶性粉末

7) 溶解性:溶于DMSO(50mM)、无水乙醇、DMF、几乎不溶于水

8) 化学结构图:


保存与运输方法

保存:-20ºC避光干燥保存,至少2年有效。

运输:冰袋运输。


注意事项

1)本品不是临床药物,只能用于科研用途,不能用于诊断或临床用途。

2)本品是一种肿瘤促进剂,操作时做好防护措施避免任何途径的直接接触。

3)为了您的安全和健康,请穿实验服并戴一次性手套操作。


使用方法【源自文献,仅作参考】

文献1,Hudák R et al. The Phosphatase Inhibitor Calyculin-A Impairs Clot Retraction, Platelet Activation, and Thrombin Generation. Biomed Res Int. 2017:9795271.PMID: 28680886

体外研究:

细胞类型(Cell type):Platelet-rich plasma (PRP) sample

药物配制(Preparation):Calyculin-A (CLA) was dissolved in DMSO

实验方法(Assay):PRP (110μL) was preincubated with either HEPES buffer containing 0.5% DMSO as control or the protein phosphatase inhibitor CLA (50nM), for 30 minutes at 37°C in a water bath. After preincubation, platelets were activated either by TRAP (20μM) or by thiomersal (200mM) for 15 minutes at 37°C in a water bath. Then PRP (5μL) was stained with 5μL monoclonal CD41-PE antibody and 5μL Annexin-V-FITC and Annexin-V binding buffer (1x concentrate) was added to examine the PS-expression of the platelets.

文献2,Blank T et al. The phosphoprotein DARPP-32 mediates cAMP-dependent potentiation of striatal N-methyl-D-aspartate responses. Proc Natl Acad Sci U S A. 1997 Dec 23;94(26):14859-64. PMID: 9405704

体外研究:

细胞类型(Cell type):Xenopus Oocytes

药物配制(Preparation):Calyculin A was prepared in 100% ethanol as a 1 mM stock solution. Immediately after dilution in distilled water to the appropriate concentration, calyculin A was microinjected into the oocytes according to the RNA injection protocol.

实验方法(Assay):The NMDA-induced currents of striatal mRNA-injected oocytes were measured before and 8 min after 1-min application of 50 μM forskolin or before and 12 min after 1-min application of 10 nM PMA. The same protocol was followed after injecting oocytes with calyculin A to a final intracellular concentration of 500 nM 60–90 min before voltage-clamping. The intracellular concentration of calyculin A was calculated by assuming standard oocytes with a volume of 0.5 μl.

文献3,Fabian L et al. Calyculin A, an enhancer of myosin, speeds up anaphase chromosome movement. Cell Chromosome. 2007 Mar 24;6:1. PMID: 17381845

体外研究:

细胞类型(Cell type):Living crane-fly spermatocytes

药物配制(Preparation):Calyculin A was dissolved in DMSO as a 1mM or 50 μM stock solution.

实验方法(Assay):Living crane-fly spermatocytes were perfused with insect Ringer's solution or with Calyculin A in insect Ringer's solution, at final concentrations of 0.5 μM, 100 nM, 50 nM, 20 nM, 10 nM or 5 nM, prepared from a 1 mM or a 50 μM Calyculin A stock in DMSO. Results showed that concentrations of 5 nM and 10 nM had no effect on anaphase chromosome movement, 20 nM had inconsistent effects, and 50 nM had consistent effects. Thus we used 50 nM for most of the experiments.


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