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Merck
CN

SML1916

Sigma-Aldrich

马里佐米

≥95% (HPLC), (Salinospora tropica)

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别名:
(1R,4R,5S)-4-(2-氯乙基)-1-[(S)-(1S)-2-环己烯-1-基羟甲基] -5-甲基-6-氧杂-2-氮杂双环[3.2. 0]庚烷-3,7-二酮, NPI-0052, 盐孢酰胺A
经验公式(希尔记法):
C15H20ClNO4
分子量:
313.78
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

生物来源

(Salinospora tropica)

检测方案

≥95% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

运输

wet ice

储存温度

−20°C

InChI

1S/C15H20ClNO4/c1-14-10(7-8-16)12(19)17-15(14,13(20)21-14)11(18)9-5-3-2-4-6-9/h3,5,9-11,18H,2,4,6-8H2,1H3,(H,17,19)/t9-,10+,11+,14+,15+/m1/s1

InChI key

NGWSFRIPKNWYAO-SHTIJGAHSA-N

应用

Marizomib作为蛋白酶体抑制剂已用于:
  • 研究其对胶质母细胞瘤细胞系的影响
  • 分析其对鳉鱼脑老化的影响
  • 检测其对多发性骨髓瘤细胞中蛋白激酶B(PKB/AKT)水平的影响

生化/生理作用

Marizomib是一种具有抗癌活性的第二代蛋白酶体抑制剂。Marizomib能够不可逆地结合并有效抑制所有三种20S蛋白酶体亚基。
Marizomib(马里佐米)属于天然产物,是一种海洋生物来源的β-内酯-γ-内酰胺。它具有对血液和实体恶性肿瘤的治疗作用。它参与胱天蛋白酶3、8和9活化,增加活性氧(ROS)和促进细胞凋亡。Marizomib可穿过血脑屏障,是治疗原发脑肿瘤的潜力药物。它具有抗肿瘤特性。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Nancy Levin et al.
British journal of haematology, 174(5), 711-720 (2016-05-11)
Proteasome inhibitors (PIs) are highly active in multiple myeloma (MM) but resistance is commonly observed. All clinical stage PIs effectively inhibit chymotrypsin-like (CT-L) activity; one possible mechanism of resistance is compensatory hyperactivation of caspase-like (C-L) and trypsin-like (T-L) subunits, in
A M Rajan et al.
Blood cancer journal, 6(7), e451-e451 (2016-07-30)
The treatment of multiple myeloma (MM) is rapidly evolving. In the United States, four drugs (panobinostat, ixazomib, daratumumab and elotuzumab) were approved for the treatment of MM in 2015. As a result of improved diagnosis and therapy, there has been
Kaijun Di et al.
Neuro-oncology, 18(6), 840-848 (2015-12-19)
The proteasome plays a vital role in the physiology of glioblastoma (GBM), and proteasome inhibition can be used as a strategy for treating GBM. Marizomib is a second-generation, irreversible proteasome inhibitor with a more lipophilic structure that suggests the potential
B C Potts et al.
Current cancer drug targets, 11(3), 254-284 (2011-01-21)
The proteasome has emerged as an important clinically relevant target for the treatment of hematologic malignancies. Since the Food and Drug Administration approved the first-in-class proteasome inhibitor bortezomib (Velcade) for the treatment of relapsed/refractory multiple myeloma (MM) and mantle cell
Erika Kelmer Sacramento et al.
Molecular systems biology, 16(6), e9596-e9596 (2020-06-20)
A progressive loss of protein homeostasis is characteristic of aging and a driver of neurodegeneration. To investigate this process quantitatively, we characterized proteome dynamics during brain aging in the short-lived vertebrate Nothobranchius furzeri combining transcriptomics and proteomics. We detected a

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