|(2S,2'S)-N,N'-((2S,2'S)-(己烷-1,6-二基双(氮杂二基))双(1-氧代-3,3-二苯基丙烷-1,2-二基))双 (1-((S)-2-环己基-2-((S)-2-(甲基氨基)丙酰胺基)乙酰基)吡咯烷-2-甲酰胺)|CsnPharm

CAS No.: 1001600-56-1

BV6 Catalog No. CSN17381

Synonyms: BV-6 free

BV6 is a small-molecule Smac mimetic, which antagonizes IAP and induces autoubiquitination and subsequent proteasomal degradation of cIAP1 and cIAP2.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述BV6 is an IAP antagonist with Kd values of o.46nM and 1.3nM for c-IAP and XIAP, respectively. Treatment with BV-6 could cause time (5μM, 2-60min)-dependent c-IAP1 and c-IAP2 ubiquitin degradation in MDA-MB-231 cells. The loss of XIAP can be observed at 8h post treatment. BV-6 led induced caspase-dependent cell death in EVSAT and A2058 cells at concentration ranging in 8-1000nM for 24h concentration-dependently, as well as cell death in MDA-MB-231 at concentration<20nM. And this cell death by BV-6 was TNF dependent. BV-6 at 5μM induced a 15- to 30-fold increase in TNFα mRNA levels and further activated its downstream, both of canonical and noncanonical NF-κB pathways, as the phosphorylation and subsequent proteasomal degradation of IκB, time-dependent increased p52 and p100 and inhibited destabilization of NIK by BV-6 can be observed^[1]. After treatment with 10mg/kg BV6, i.p., for 4 weeks could significantly reduce the total number of lesions, the average weight and the surface area of lesions in endometriosis-like model^[2].
作用机制BV-6 can bind to the BIR domains of IAP proteins and then lead to rapid ubiquitination and proteasomal degradation of cIAPs.^[1]
动物研究
剂量
Mice: 10 mg/kg^[2] (i.p.); 1 mg/kg, 3 mg/kg^[3] (i.v.)

给药途径
i.p., i.v.
临床研究

动物研究
剂量	Mice: 10 mg/kg^[2] (i.p.); 1 mg/kg, 3 mg/kg^[3] (i.v.)
给药途径	i.p., i.v.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02200718	Multiple Sclerosis	Phase 1	Not yet recruiting	November 2019	United States, Oregon ... more >> Multiple Sclerosis Center Oregon Health & Science University Not yet recruiting Portland, Oregon, United States, 97239 Contact: Richard M Bartholomew, PhD 858-414-4664 Richardmbartholomew@gmail.com Principal Investigator: Dennis Bourdette, MD F.A.A.N. Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.8295 mL
- 4.1474 mL
- 8.2948 mL
- 5 mM
- 0.1659 mL
- 0.8295 mL
- 1.6590 mL
- 10 mM
- 0.0829 mL
- 0.4147 mL
- 0.8295 mL

技术信息

CAS号

1001600-56-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C70H96N10O8

运输

蓝冰

分子量

1205.57

别名

BV-6 free

溶解度

DMSO	100.0 mg/mL (82.9 mM)

动物实验配方

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