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幹燥保存 |
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
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産品編号
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CAS NO.
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規格
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價格(元)
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Calyculin A 花萼海綿體誘癌素A
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MZ2504-25UG
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101932-71-2
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25 µg
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2062
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Calyculin A 花萼海綿體誘癌素A
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MZ2504-50UG
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101932-71-2
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50
µg
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3262
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Calyculin
A 花萼海綿體誘癌素A
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MZ2504-100UG
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101932-71-2
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100
µg
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4862
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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.
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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.
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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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|
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— —Written/Edited by V.
Shallan【版權歸MKBio懋康所有】
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