MZ2504 Calyculin A 花萼海绵体诱癌素A
2021-08-12 16:23  点击:347
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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

1446

Calyculin A 花萼海绵体诱癌素A

MZ2504-50UG

101932-71-2

50 µg

2486

Calyculin A 花萼海绵体诱癌素A

MZ2504-100UG

101932-71-2

100 µg

3946

产品描述

花萼海绵体诱癌素A(Calyculin A,CAS NO:101932-71-2)zui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:

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, Plaet Activation, and Thrombin Generation. Biomed Res Int. 2017:9795271. PMID: 28680886

体外研究:

细胞类型(Cell type):Plaet-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, plaets 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 plaets.

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 ethanol as a 1 mM stock solution. Immediay 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.

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Calyculin A 花萼海绵体诱癌素A
Calyculin A 花萼海绵体诱癌素A
Calyculin A 花萼海绵体诱癌素A

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