SM-164 (XIAP抑制剂)
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产品编号 SC0114-10mM
数量
¥ 823.00
产品包装:
10mM×0.2ml 5mg 25mg
产品简介
使用说明
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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):

酶活性检测实验
方法 N/A
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。 

使用说明:
1. 收到产品后请立即按照说明书推荐的条件保存。使用前可以在2,000-10,000g离心数秒,以使液体或粉末充分沉降至管底后再开盖使用。
2. 对于10mM溶液,可直接稀释使用。对于固体,请根据本产品的溶解性及实验目的选择相应溶剂配制成高浓度的储备液(母液)后使用。
3. 具体的最佳工作浓度请参考本说明书中的体外、体内研究结果或其它相关文献,或者根据实验目的,以及所培养的特定细胞和组织,通过实验进行摸索和优化。
4. 不同实验动物依据体表面积的等效剂量转换表请参考如下网页:http://www.beyotime.com/support/animal-dose.htm
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