Boc-D-FMK
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Boc-D-FMK是一种细胞通透性的广谱caspase抑制剂,可完全抑制肿瘤坏死因子α的促凋亡效应,IC50值为39 μM[1]。
Boc-D-FMK可减弱核因子活化B细胞κ轻链增强子(NF-kB)的激活,抑制免疫球蛋白κ轻链基因增强子抑制蛋白α(IkBα)亚基的磷酸化作用,并抑制TNF诱导的细胞间粘附分子1(ICAM-1)和血管细胞黏着分子1(VCAM-1)的表达[2]。
此外,在胆总管结扎大鼠模型中, Boc-D-FMK可有效减少肝细胞凋亡,提高存活率[3]。
参考文献:
[1] Cowburn AS, White JF, Deighton J, Walmsley SR, Chilvers ER. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species. Blood. 2005 Apr 1;105(7):2970-2. Epub 2004 Nov 30.
[2] Wu X, Guo R, Chen P, Wang Q, Cunningham PN. TNF induces caspase-dependent inflammation in renal endothelial cells through a Rho- and myosin light chain kinase-dependent mechanism. Am J Physiol Renal Physiol. 2009 Aug;297(2):F316-26. doi: 10.1152/ajprenal.00089.2009. Epub 2009 May 6.
[3] Sheen-Chen SM, Hung KS, Eng HL. Effect of Boc-D-Fmk on hepatocyte apoptosis after bile duct ligation in rat and survival rate after endotoxin challenge. J Gastroenterol Hepatol. 2008 Aug;23(8 Pt 1):1276-9. doi: 10.1111/j.1440-1746.2008.05368.x. Epub 2008 Mar 27.
Storage | Store at -20°C |
M.Wt | 263.26 |
Cas No. | 187389-53-3,634911-80-1 |
Formula | C11H18FNO5 |
Synonyms | Caspase Inhibitor III, Boc-Asp(OMe)-FMK, Boc-D(OMe)-FMK, Caspase3-Inhibitor BOC-D-FMK, Boc-Asp(OMe)-fluoromethylketone |
Solubility | insoluble in H2O; ≥11.65 mg/mL in DMSO; ≥41.65 mg/mL in EtOH |
Chemical Name | methyl 5-fluoro-3-[(2-methylpropan-2-yl)oxycarbonylamino]-4-oxopentanoate |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)OC(=O)NC(CC(=O)OC)C(=O)CF |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
C57BL/6小鼠肾内皮细胞 |
溶解方法 |
在DMSO中的溶解度> 11.65 mg/mL。为了获得更高浓度,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 |
100μM孵育3小时 |
应用 |
经4小时的TNF处理所造成的小鼠肾内皮细胞凋亡能够极大地被广谱caspase抑制剂Boc-D-fmk所抑制,caspase-3 抑制剂 z-DQMD-fmk也能达到同样的效果。此外,广谱caspase抑制剂Boc-D-fmk也能显著抑制TNF诱导的ICAM-1和VCAM-1mRNA的表达。 |
动物实验 [2]: | |
动物模型 |
雄性SD大鼠 |
剂量 |
腹腔给药1.5 mg/kg |
应用 |
与假手术组相比,胆总管结扎并给药ZFA-fmk显著增加肝细胞的凋亡。与OBZFA组相比,Boc-D-FMK治疗能显著缓解在OBBOC-D组出现的肝细胞凋亡。同时研究发现肝细胞凋亡程度在OBBOC-D处理组以及假手术组(SHAM)未有差别。经内毒素处理后,SHAM、OBBOC-D 组以及 OBZFA 组的48小时生存率分别为100%、 87.5% 和 62.5%。 |
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] Wu X, Guo R, Chen P, Wang Q, Cunningham PN. TNF induces caspase-dependent inflammation in renal endothelial cells through a Rho- and myosin light chain kinase-dependent mechanism. Am J Physiol Renal Physiol. 2009 Aug;297(2):F316-26. doi: 10.1152/ajprenal.00089.2009. Epub 2009 May 6. [2] Sheen-Chen SM, Hung KS, Eng HL. Effect of Boc-D-Fmk on hepatocyte apoptosis after bile duct ligation in rat and survival rate after endotoxin challenge. J Gastroenterol Hepatol. 2008 Aug;23(8 Pt 1):1276-9. doi: 10.1111/j.1440-1746.2008.05368.x. Epub 2008 Mar 27. |
Description | BOC-D-FMK是一种新型caspase-3抑制剂。 | |||||
靶点 | Caspase | |||||
IC50 |
质量控制和MSDS
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