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Salinosporamide A (NPI-0052, Marizomib)

现货
Catalog No.
A4010
20S蛋白酶体抑制剂
组合的产品项目
规格价格库存 数量
100ug
¥ 2,405.00
Ship with 10-15 days

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Background

Salinosporamide A is a potent inhibitor of 20S proteasome with IC50 value of 1.3 nM [1].

Salinosporamide A was isolated from the crude extract of a Salinospora strain CNB-392. It showed potent anti-tumor activity with an IC50 value of 11 ng/mL in HCT-116 cells. It also exerted a mean GI50 value of less than 10 nM in the NCI’s 60 cell line-panel. Among these cell lines, Salinosporamide A showed the greatest potent efficacies in NCI-H226, SF-539, SK-MEL-28 and MDA-MB-435 cells. Salinosporamide A inhibited the purified 20S proteasome with IC50 value of 1.3 nM. It was about 35-fold more potent than the first discovered specific proteasome inhibitor, omuralide [1].

References:
[1] Feling R H, Buchanan G O, Mincer T J, et al. Salinosporamide A: a highly cytotoxic proteasome inhibitor from a novel microbial source, a marine bacterium of the new genus Salinospora. Angewandte Chemie International Edition, 2003, 42(3): 355-357.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt313.78
Cas No.437742-34-2
FormulaC15H20ClNO4
Synonymssalinosporamide A, MARIZOMIB, NPI-0052, (-)-Salinosporamide A
SolubilitySoluble in DMSO
Chemical Name(1S,2R,5R)-2-(2-chloroethyl)-5-[(S)-[(1S)-cyclohex-2-en-1-yl]-hydroxymethyl]-1-methyl-7-oxa-4-azabicyclo[3.2.0]heptane-3,6-dione
SDFDownload SDF
Canonical SMILESCC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl
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

人MM细胞系(MM.1S、INA-6、RPMI-8226、MM.1R、KMS12PE和U266)

溶解方法

溶于DMSO。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

24 h;2 nM

应用

人MM细胞系用lenalidomide预处理24小时,再加入NPI-0052处理24小时后用MTT实验评估细胞活力。在所有细胞系中,与单独给药组相比,低剂量NPI-0052和lenalidomide联合给药显著减少所有细胞系的细胞活力(P<0.05;n=3)。这些数据表明,NPI-0052和lenalidomide具有协同抗MM的活性。

动物实验[2]:

动物模型

CB-17 SCID-雄性小鼠

剂量

0.15 mg/kg;i.v.

应用

在MM.1S肿瘤小鼠中,NPI-0052(0.15 mg/kg;i.v.)每周两次连续给药3周后测量肿瘤体积。与对照组相比,NPI-0052显著减少肿瘤生长(P=0.005),无任何毒性作用,体重和整体外观均无明显变化。NPI-0052处理后的5-7天显著抑制肿瘤中蛋白酶体的作用,具有抗MM活性。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Chauhan D, Singh A V, Ciccarelli B, et al. Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma[J]. Blood, 2010, 115(4): 834-845.

[2] Singh A V, Palladino M A, Lloyd G K, et al. Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI‐0052 (marizomib) in a human plasmacytoma xenograft murine model[J]. British journal of haematology, 2010, 149(4): 550-559.

生物活性

描述 Salinosporamide A (NPI-0052, Marizomib)是一种新型海生的蛋白酶体抑制剂,在人红细胞20S蛋白酶体中,抑制CT-L、C-L和T-L蛋白酶体活性,EC50为3.5 nM、430 nM和28 nM。
靶点 CT-L (EC50) C-L (EC50) T-L (EC50)      
IC50 3.5 nM 430 nM 28 nM      

质量控制

质量控制和MSDS

批次:

化学结构

Salinosporamide A (NPI-0052, Marizomib)