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Calyculin A 花萼海綿體誘癌素A
目錄号 MZ2504-100UG 售價 4862.00元
規格 100 µg 運輸溫度 冰袋
其他名稱 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 保存溫度 -20ºC避光(guāng)幹燥保存
CAS号 101932-71-2 有效期 2年(nián)
應用 蛋白(bái)磷酸酶1(PP1)和蛋白(bái)磷酸酶2A(PP2A)抑制劑 訂購數量
産品簡介:

Calyculin A 花萼海綿體誘癌素A


産品标簽

Calyculin A;Okadaic acid 岡田軟海綿酸;Protein phosphatase 1 (PP1);Protein phosphatase 2A (PP2A) ;Tumor Promoter 腫瘤促進劑;CAS NO:101932-71-2;


産品信息

産品名稱

産品編号

CAS NO.

規格             

價格(元)   

Calyculin A 花萼海綿體誘癌素A    

MZ2504-25UG        

101932-71-2   

25 µg

2060

Calyculin A 花萼海綿體誘癌素A

MZ2504-50UG

101932-71-2

50 µg

3262

Calyculin A 花萼海綿體誘癌素A

MZ2504-100UG

101932-71-2

100 µg

4862


産品描述

花萼海綿體誘癌素A(Calyculin A,CAS NO:101932-71-2)最初是從(cóng)海綿Disodermia calyx中分離到(dào)的一(yī)種海洋毒素,是一(yī)種具細胞滲透性、有效和選擇性的蛋白(bái)磷酸酶1(PP1,IC50=0.3-0.7 nM)和蛋白(bái)磷酸酶2A(PP2A,IC50=0.5-1.0 nM)抑制劑。對PP2B和PP2C的選擇性>10,000,000倍。對酸性或堿性磷酸酶或磷酸-酪氨酸蛋白(bái)磷酸酶無抑制。Calyculin A抑制平滑肌肌球蛋白(bái)B内源性磷酸酶的活性,誘導肌肉纖維收縮,并伴随細胞質遊離Ca2+水(shuǐ)平提高(gāo)。花萼海綿體誘癌素A還(hái)是一(yī)種非佛波類的腫瘤促進劑。與小(xiǎo)鼠皮膚上(shàng)的蛋白(bái)磷酸酶結合,誘導鳥氨酸脫羧酶(ODC)活性,進而促進腫瘤生(shēng)長(cháng)。


産品特性

1) CAS NO:101932-71-2

2) 化學名: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) 純度:≥98%

6) 外觀:透明薄膜或白(bái)色結晶性粉末

7) 溶解性:溶于DMSO(50mM)、無水(shuǐ)乙醇、DMF、幾乎不溶于水(shuǐ)

8) 化學結構圖:


保存與運輸方法

保存:-20ºC避光(guāng)幹燥保存,至少2年(nián)有效。

運輸:冰袋運輸。


注意事(shì)項

1)本品不是臨床藥物(wù),隻能(néng)用于科研用途,不能(néng)用于診斷或臨床用途。

2)本品是一(yī)種腫瘤促進劑,操作時做好防護措施避免任何途徑的直接接觸。

3)為(wèi)了您的安全和健康,請穿實驗服并戴一(yī)次性手套操作。


使用方法【源自(zì)文獻,僅作參考】

文獻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

體外研究:

細胞類型(Cell type):Platelet-rich plasma (PRP) sample

藥物(wù)配制(Preparation):Calyculin-A (CLA) was dissolved in DMSO

實驗方法(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.

文獻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

體外研究:

細胞類型(Cell type):Xenopus Oocytes

藥物(wù)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.

實驗方法(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.

文獻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

體外研究:

細胞類型(Cell type):Living crane-fly spermatocytes

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

實驗方法(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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