製品名
マリゾミブ, ≥95% (HPLC), (Salinospora tropica)
SMILES string
ClCC[C@@H]1[C@@]2(OC(=O)[C@@]2(NC1=O)[C@@H](O)[C@H]3CCCC=C3)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
biological source
(Salinospora tropica)
assay
≥95% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
shipped in
wet ice
storage temp.
−20°C
Quality Level
関連するカテゴリー
Application
マリゾミブは、下記で、プロテアソーム阻害薬として使用されています:
- 神経膠芽腫細胞株に対する影響を検討するため
- メダカの脳の加齢に対する影響を解析するため
- 多発性骨髄腫細胞においてプロテインキナーゼB(PKB/AKT)濃度に対する影響を試験するため
Biochem/physiol Actions
マリゾミブは天然物で、海洋由来のβ-ラクトン-γ-ラクタムです。血液悪性腫瘍および固形悪性腫瘍に対し治療効果があります。カスパーゼ-3、-8、および -9の活性化に関与しており、活性酸素種(ROS)を増加させ、アポトーシスを促進します。マリゾミブは血液脳関門を通過でき、原発性脳腫瘍を治療できる可能性があります。抗腫瘍特性があります。
マリゾミブは抗がん作用を有する第2世代のプロテアソーム阻害薬です。
マリゾミブは抗がん作用を有する第2世代のプロテアソーム阻害薬です。マリゾミブは3種類の20Sプロテアソームサブユニットすべてに不可逆的に結合し、強力に阻害します。
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
Marizomib activity as a single agent in malignant gliomas: ability to cross the blood-brain barrier.
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
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
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
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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