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(3S)-3-[[叔丁氧羰基]氨基]-5-氟-4-氧代-戊酸甲酯

用途

Boc-Asp(OME)-氟甲基酮是一种广泛的caspase抑制剂,可抑制Fas介导的吞噬和氧化破裂抑制,但不影响IL-8的趋化活性[1][2]。

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名称

[ CAS 号 ]:
187389-53-3

[ 中文名 ]:
(3S)-3-[[叔丁氧羰基]氨基]-5-氟-4-氧代-戊酸甲酯

[ 英文名 ]:
Boc-D-FMK

[英文别名 ]:

caspase inhibitor3

生物活性

[ 描述 ]:

Boc-Asp(OME)-氟甲基酮是一种广泛的caspase抑制剂,可抑制Fas介导的吞噬和氧化破裂抑制,但不影响IL-8的趋化活性[1][2]。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 胱天蛋白酶

研究领域 >> 炎症/免疫

[ 靶点 ]

Caspase

[体外研究]

Boc-Asp(OME)-氟甲基酮(100μM；30分钟；多形核白细胞)可防止Fas诱导的自发凋亡(−CH-11[1]。Boc-Asp(OME)-氟甲基酮(20μM；5小时；J774.1/JA-4细胞)显著增加LDH释放[2]。

[参考文献]

[1]. Paunel-Görgülü A, et al. Stimulation of Fas signaling down-regulates activity of neutrophils from major trauma patients with SIRS. Immunobiology. 2011;216(3):334-342.

[2]. Koike A, et al. Pan-caspase inhibitors induce necroptosis via ROS-mediated activation of mixed lineage kinase domain-like protein and p38 in classically activated macrophages. Exp Cell Res. 2019;380(2):171-179.

物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
383.5±37.0 °C at 760 mmHg

[ 分子式 ]:
C₁₁H₁₈FNO₅

[ 分子量 ]:
263.263

[ 闪点 ]:
185.7±26.5 °C

[ 精确质量 ]:
263.116913

[ PSA ]:
81.70000

[ LogP ]:
1.91

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.440

[ 储存条件 ]:
-20°C，密闭，干燥

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2924199090

海关

[ 海关编码 ]: 2924199090

[ 中文概述 ]:
2924199090. 其他无环酰胺（包括无环氨基甲酸酯)(包括其衍生物及盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924199090. other acyclic amides (including acyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

文献

C1 Domain-targeted isophthalate derivatives induce cell elongation and cell cycle arrest in HeLa cells.

PLoS ONE 6 , e20053, (2011)

Diacylglycerol (DAG)-mediated signaling pathways, such as those mediated by protein kinase C (PKC), are central in regulating cell proliferation and apoptosis. DAG-responsive C1 domains are therefore ...

Caspase inhibitors promote the survival of avulsed spinal motoneurons in neonatal rats.

Neuroreport 12 , 541, (2001)

Following ventral root avulsion in neonatal animals, the degeneration of spinal motoneurons occurs by an apoptotic-like morphological pathway. In adult animals, however, the mechanism of degeneration ...

The maternal-effect gene cellular island encodes aurora B kinase and is essential for furrow formation in the early zebrafish embryo.

PLoS Genet. 5 , e1000518, (2009)

Females homozygous for a mutation in cellular island (cei) produce embryos with defects in cytokinesis during early development. Analysis of the cytoskeletal events associated with furrow formation re...

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