化学信息：
|
化学名
|
(3S,6S,10aS)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl] amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)
|
|
简称
|
SM-164
|
|
别名
|
SM 164, SM164
|
|
中文名
|
N/A
|
|
化学式
|
C62H84N14O6
|
|
分子量
|
1121.42
|
|
CAS号
|
957135-43-2
|
|
纯度
|
-
|
|
溶剂/溶解度
|
DMSO 12mg/ml
|
|
溶液配制
|
5mg加入0.45ml DMSO，或者每11.21mg加入1ml DMSO，配制成10mM溶液。SC0002-10mM用DMSO配制。
|
|
|
生物信息：
|
产品描述
|
SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1nM, respectively
|
|
信号通路
|
Apoptosis
|
|
靶点
|
XIAP
|
cIAP-1
|
cIAP-2
|
-
|
-
|
|
IC50
|
0.56nM(Ki)
|
0.31nM(Ki)
|
1.1nM(Ki)
|
-
|
-
|
|
体外研究
|
SM-164 induced complete cIAP-1 degradation, it displayed weak inhibitory effects on the viability of HCC cells. Nevertheless, SM-164 considerably potentiated Apo2 ligand or TNF-related apoptosis-inducing ligand (APO2L/TRAIL)- and Doxorubicin-mediated anticancer activity in HCC cells. Mechanistic studies demonstrated that SM-164 in combination with chemotherapeutic agents resulted in enhanced activation of caspases-9, -3 and cleavage of poly ADP-ribose polymerase (PARP), and also led to decreased AKT activation. Although SM-164 is modestly more effective than SM-122 in induction of cIAP-1/2 degradation, SM-164 is 1,000 times more potent than SM-122 as an inducer of apoptosis in tumor cells, which is attributed to its much higher potency in binding to and antagonizing XIAP. SM-164 radiosensitization in sensitive cells was associated with NF-κB activation and TNFα secretion, followed by activation of caspase-8 and -9, leading to enhanced apoptosis.
|
|
体内研究
|
SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. SM-164 also radiosensitized human tumor xenograft while causing minimal toxicity.
|
|
临床实验
|
N/A
|
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
|
细胞实验
|
|
细胞系
|
N/A
|
|
浓度
|
N/A
|
|
处理时间
|
N/A
|
|
方法
|
N/A
|
|
动物实验
|
|
动物模型
|
N/A
|
|
配制
|
N/A
|
|
剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Lu J, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 2008 Nov 15; 68(22):9384-93.
2. Yang J, et al. Radiosensitization of head and neck squamous cell carcinoma by a SMACmimetic compound, SM-164, requires activation of caspases. Mol Cancer Ther. 2011 Apr; 10(4):658-69.
3. Zhang S, et al. Smac mimetic SM-164 potentiates APO2L/TRAIL-and doxorubicin-mediated anticancer activity in human hepatocellular carcinoma cells. PLoS One. 2012; 7(12):e51461.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SC0114-10mM
|
SM-164 (XIAP抑制剂)
|
10mM×0.2ml
|
|
SC0114-5mg
|
SM-164 (XIAP抑制剂)
|
5mg
|
|
SC0114-25mg
|
SM-164 (XIAP抑制剂)
|
25mg
|
|
-
|
说明书
|
1份
|
保存条件：
-20℃保存，至少一年有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
