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Salinosporamide A (NPI-0052)

Dangerous Goods

CAS number:437742-34-2    molecular formula:C15H20ClNO4

overview

compound introduction

Information Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) is a novel marine derived proteasome inhibitor which inhibitsCT-L β5,C-L β1, andT-L β2proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM. Targets CT-L β5 (Cell-free assay); T-L β2 (Cell-free assay); C-L β1 (Cell-free assay) 3.5 nM; 28 nM; 430 nM In vitro Marizomib inhibits the proteasome activity, proliferation, and invasion of glioma cells. Meanwhile, free radical production and apoptosis induced by marizomib can be blocked by antioxidant N-acetyl cysteine. In vivo In animal studies, marizomib distributes into the brain at 30% of blood levels in rats and significantly inhibits (>30%) baseline chymotrypsin-like proteasome activity in brain tissue of monkeys. Encouragingly, the immunocompromised mice, intracranially implanted with glioma xenografts, survives significantly longer than the control animals when treated with marizomib. Cell Research(from reference) Cell lines:The human glioma cell lines U-251 MG and D-54 MG Concentrations:60 nM Incubation Time:2 h, 24 h

Specs

Chinese alias-
English alias6-OXA-2-AZABICYCLO(3.2.0)HEPTANE-3,7-DIONE, 4-(2-CHLOROETHYL)-1-((S)-(1S)-2-CYCLOHEXEN-1-YLHYDROXYMETHYL)-5-METHYL-, (1R,4R,5S)- | NPI 0052 | (1R,4R,5S)-4-(2-chloroethyl)-1-[(S)-(1S)-cyclohex-2-en-1-yl(hydroxy)methyl]-5-methyl-6-oxa-2-azabicyclo[3.2.0]hep
CAS number437742-34-2molecular formulaC15H20ClNO4
molecular weight313.78 g/molExact mass≥99%
PSA75.600 Ųlogp1.8

numbering system

No numbering system information yet

physicochemical properties

No physical and chemical property information yet

Safety information

pictogram:
GHS08 , GHS07
Signal word:
Danger
Hazard Statement:
H315: 引起皮肤刺激 H372: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子
Statement of Preventive Measures:
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P321: 特殊处理(请参阅此标签上的...)。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P203: 使用前,获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心,请就医。
RTECS:
RN6803500

Production methods and uses

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Related

upstream information

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downstream information

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MSDS

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