Kinasechem是来自英国的专业的抑制剂供应商，提供覆盖几百个激酶靶点的抑制剂。 Kinasechem的产品涉及绝大多数的信号通路研究以及癌症研究，包括： PI3K-Akt signaling pathway； MAPK signaling pathway; apoptosis(凋亡)； DNA damage( DNA 损伤) RTK(受体酪氨酸激酶） 等抑制剂在生命科学研究领域的应用非常广泛。在信号通路以及癌症研究方面，很多地方需要用到抑制剂来阻抑信号通路。目前，在HIV的研究，抗感染，心血管疾病，老年痴呆症（阿兹海默症），甚至糖尿病的研究中，都会使用到抑制剂。 1、 抑制剂的一般使用方法：（1）细胞实验将抑制剂溶解于DMSO, 乙醇或者水中，稀释到需要的浓度。一般孵育48小时，也有孵育2周的实验。（2）动物实验小鼠模型：以注射为主。大鼠模型：以口服为主。（3）抗药性筛选实验长期孵育，递增性增加浓度。 2、抑制剂的几个重要参数： IC50(半抑制浓度) 指抑制剂降低对应激酶的活性到原来活性的一半的浓度。 IC50是抑制剂一个重要的指标，一般而言，IC50越小，抑制能力越强。 EC50 指加入抑制剂后，细胞死亡一半所需的浓度。 抑制剂选择性抑制剂有多重抑制剂，指同时抑制多个靶点的抑制剂。有高选择性抑制剂，仅仅抑制某些激酶的某个亚型或者结构域。比如，有的抑制剂仅仅抑制PI3K这个激酶的gamma亚型。
Information

SKU:K1200		M. Wt:561.71
Formula:C32H43N5O4		Solubility:DSMO 112 mg/mL Water <1 mg/ml Ethanol 112 mg/mL
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1071992-99-8
Chemical Name(5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxo- decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide

Biological Activity

Description	AT-406(SM-406) can inhibit XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM.
Targets	XIAP	cIAP1	cIAP2
IC50	66.4 nM (Ki)	1.9 nM(Ki)	5.1 nM(Ki)
In vitro	AT-406(SM-406) is a novel, potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). AT-406(SM-406) can inhibit XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM. AT-406(SM-406) can induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. In ovarian cancer cells, AT-406(SM-406) shows therapeutic efficacy and mechanism of action in 60% of human ovarian cancer cell lines. AT-406 induced apoptosis is correlated with its ability to down-regulate XIAP whereas AT-406 induces cIAP1 degradation in both AT-406 sensitive and resistance cell lines.
IN vivo	In vivo, AT-406(SM-406) inhibits ovarian cancer progression and shows therapeutic potential for patients with inherent or acquired platinum resistance.In the combination with carboplatin, AT-406(SM-406) shows therapeutic efficacy.In vivo, AT-406(SM-406) enhances the carboplatin-induced ovarian cancer cell death and increases survival of the experimental mice by making ovarian cancer cells more sensitive to carboplatin.