切换导航

Okadaic acid

现货
Catalog No.
A4540
蛋白磷酸酶1抑制剂
组合的产品项目
规格价格库存 数量
50ug
¥ 960.00
Ship with 10-15 days
100ug
¥ 1,820.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Okadaic acid is a potent inhibitor of protein phosphatase 1/2A with IC50 values of 19 nM and 0.2 nM for protein phosphatase 1 and protein phosphatase 2A, respectively [1].

Protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) are two major mammalian serine/threonine protein phosphatases and are activated in response to Ca2+ cascades as well as increased protein kinase A activity [2].

In confluent rabbit lens epithelial cells (RLECs), okadaic acid (100 nM) significantly induced cell apoptosis. Also, okadaic acid induced the expression of p53 and bax, which are necessary for the apoptotic programs. In N/N1003A cells, okadaic acid (10 nM) decreased total phosphatase activity by 20% and mainly inhibited PP-2A activity, while okadaic acid (100 nM) reduced 81% total phosphatase activity and inhibited PP-1 and PP-2A activity [3].

In the rat striatum, okadaic acid (0.005, 0.05 and 0.5 nM) increased Elk-1 and CREB phosphorylation and c-Fos immunoreactivity in a dose-dependant way. Also, okadaic acid (0.05 and 0.5 nM) increased c-fos mRNA expression in a dose-dependent way [2].

References:
[1].  Holmes CF. Liquid chromatography-linked protein phosphatase bioassay; a highly sensitive marine bioscreen for okadaic acid and related diarrhetic shellfish toxins. Toxicon, 1991, 29(4-5): 469-477.
[2].  Choe ES, Parelkar NK, Kim JY, et al. The protein phosphatase 1/2A inhibitor okadaic acid increases CREB and Elk-1 phosphorylation and c-fos expression in the rat striatum in vivo. J Neurochem, 2004, 89(2): 383-390.
[3].  Li DW, Fass U, Huizar I, et al. Okadaic acid-induced lens epithelial cell apoptosis requires inhibition of phosphatase-1 and is associated with induction of gene expression including p53 and bax. Eur J Biochem, 1998, 257(2): 351-361.

Chemical Properties

Physical AppearanceA solution in ethanol
StorageDesiccate at -20°C
M.Wt805.01
Cas No.78111-17-8
FormulaC44H68O13
SolubilitySoluble in DMSO
Chemical Name9,10-Deepithio-9,10-didehydroacanthifolicin
SDFDownload SDF
Canonical SMILESCC1CCC2(CCCCO2)OC1C(C)CC(C3C(=C)C(C4C(O3)CCC5(O4)CCC(O5)C=CC(C)C6CC(=CC7(O6)C(CCC(O7)CC(C)(C(=O)O)O)O)C)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

兔晶状体上皮细胞,N/N1003A细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10-100 nM,0-24 h

应用

在融合性的兔子晶状体上皮细胞(RLECs)中,Okadaic acid(100 nM)孵育3-24h显著诱导细胞凋亡。此外,Okadaic acid诱导凋亡程序所必需的p53和bax的表达。在N/N1003A细胞中,Okadaic acid(10 nM)将总磷酸酶的活性降低20%,主要抑制PP-2A活性,而Okadaic acid(100 nM)降低总磷酸酶活性的81%,并抑制PP-1和PP-2A活性。

动物实验 [2]:

动物模型

成年雄性Wistar大鼠

给药剂量

0–10 mg/kg,30 min,注射套管

应用

肠内输注Okadaic acid(0.005、0.05和0.5 nmol)以剂量依赖的方式增加注射的背纹纹状体中CREB和Elk-1的磷酸化以及c-Fos的免疫反应性。Okadaic acid(0.05和0.5 nM)以剂量依赖的方式增加背侧纹状体中c-fos mRNA的表达。Okadaic acid(0.05和0.5 nmol)以剂量依赖的方式显著增加纹状体中的c-fos mRNA杂交信号。Okadaic acid (0.05 nmol)显著增加pCREB和pElk-1。Okadaic acid(10 nM)抑制PP-2A活性,Okadaic acid(100 nM)抑制PP-2A和PP-1活性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Li DW, Fass U, Huizar I, et al. Okadaic acid-induced lens epithelial cell apoptosis requires inhibition of phosphatase-1 and is associated with induction of gene expression including p53 and bax. Eur J Biochem, 1998, 257(2): 351-361.

[2]. Choe ES, Parelkar NK, Kim JY, et al. The protein phosphatase 1/2A inhibitor okadaic acid increases CREB and Elk-1 phosphorylation and c-fos expression in the rat striatum in vivo. J Neurochem, 2004, 89(2): 383-390.

质量控制

质量控制和MSDS

批次:

化学结构

Okadaic acid