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Bioymifi

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Chemical Structure| 1420071-30-2 同义名 : DR5 Activator
CAS号 : 1420071-30-2
货号 : A130673
分子式 : C22H12BrN3O4S
纯度 : 98%
分子量 : 494.317
MDL号 : MFCD28118988
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 12 mg/mL(24.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 TNF-related apoptosis-inducing ligand (TRAIL, APO2L) is a member of the TNF cytokine superfamily,and is involved in pathogenesis of and/or possible treatment approaches for a variety of diseases including but not limited to cancer, obesity, diabetes, rheumatoid arthritis, and neurodegenerative diseases[2]. TRAIL secreted from natural killer (NK) cells binds to death receptors (DR4 or DR5). Bioymifi is an activator of the TRAIL receptor DR5 for cancer therapy. Bioymifi bound the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM[3]. Human glioblastoma cells T98G cells, lung cancer cell lines H460 and H1155, the cervical cancer cell line HeLa, the osteosarcoma cell line U2OS, the pancreatic carcinoma cell line Miapaca and the colon cancer cell line HT29 showed single-agent sensitivity to bioymifi which is dependent on caspase-8[3]. Caspase-3 was rapidly activated as early as 2 h after bioymifi treatment (5 μM) of T98G cells and its activity was markedly increased after 8 h of treatment[3].
作用机制 Bioymifi bound the extracellular domain (ECD) of DR5.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.11mL

2.02mL

1.01mL

20.23mL

4.05mL

2.02mL

参考文献

[1]Wang G, Wang X, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. Nat Chem Biol. 2013 Feb;9(2):84-9.

[2]Mert U, Sanlioglu AD. Intracellular localization of DR5 and related regulatory pathways as a mechanism of resistance to TRAIL in cancer. Cell Mol Life Sci. 2017 Jan;74(2):245-255. doi: 10.1007/s00018-016-2321-z. Epub 2016 Aug 10. PMID: 27510421.

[3]Wang G, Wang X, Yu H, Wei S, Williams N, Holmes DL, Halfmann R, Naidoo J, Wang L, Li L, Chen S, Harran P, Lei X, Wang X. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. Nat Chem Biol. 2013 Feb;9(2):84-9. doi: 10.1038/nchembio.1153. Epub 2012 Dec 23. PMID: 23292651.