
Molecular Weight: | 494.32 |
Formula: | C22H12BrN3O4S |
Purity: | ≥ 97% |
CAS#: | 1420071-30-2 |
Solubility: | DMSO up to 50 mM |
Chemical Name: | (Z)-5-(5-((3-(4-bromophenyl)-2-imino-4-oxothiazolidin-5-ylidene)methyl)furan-2-yl)isoindoline-1,3-dione |
Storage: | Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year. |
Biological Activity:
Bioymifi is a potent and selective small molecule agonist of DR5, identified by a high-throughput chemical screening for compounds that promote cell death in synergy with a small-molecule mimetic of Smac. Bioymifi directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation. Bioymifi induces caspase-8–dependent apoptosis, which occurs through a DR5-dependent extrinsic pathway but independent of TRAIL. Bioymifi is capable of acting as a single agent to induce DR5 clustering and aggregation, leading to apoptosis without the need for a Smac mimetic in a variety of cancer cell lines, even in U2OS and HT29 cell lines. Bioymifi could be a potential lead compound for the development of small-molecule TRAIL mimics targeting DR5 for cancer therapy.
How to Use:
In vitro:Bioymifi was used at 5-10 µM final concentration in vitro and in cellular assays.
In vivo:n/a
Reference:
- 1. Wang G, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. (2012) Nat Chem Biol. 9(2):84-89.
Bioymifi_spec.pdf
Bioymifi_MSDS.pdf
Products are for research use only. Not for human use.
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大多数药物在体内都是和特异性受体相互作用,改变细胞的生理生化功能而产生效应。目前已经确定的受体有30多种,根据受体存在的标准,受体可大致分为三类:
1.细胞膜受体:位于靶细胞膜上,如胆碱受体、肾上腺素受体、多巴胺受体、阿片受体等。
2.胞浆受体:位于靶细胞的胞浆内,如肾上腺皮质激素受体、性激素受体。
3.胞核受体:位于靶细胞的细胞核内,如甲状腺素受体。
另外也可根据受体的蛋白结构、信息转导过程、效应性质、受体位置等特点将受体分为四类:
1.含离子通道的受体(离子带受体):如N-型乙酰胆碱受体含钠离子通道。
2.G蛋白偶联受体:M-乙酰胆碱受体、肾上腺素受体等。
3.具有酪氨酸激酶活性的受体:如胰岛素受体。
4.调节基因表达的受体(核受体):如甾体激素受体、甲状腺激素受体等。
有些受体具有亚型,各种受体都有特定的分布部位核特定的功能,有些细胞也有多种受体。
请教各位大神,我最近在做WB,565KD的蛋白,动物组织的样品,听说样品制备需要蔗糖裂解液,请问这个是必须的嘛?用一般蛋白提取方法制备可以吗?还有电泳和转膜条件能否分享一下。不胜感激

