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  • 化合物 AT-406 HCl|T3299|TargetMol

化合物 AT-406 HCl|T3299|TargetMol

Xevinapant hydrochloride
1071992-57-8
327 1mg 起订
上海 更新日期:2024-09-30

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 AT-406 HCl
英文名称:
Xevinapant hydrochloride
CAS号:
1071992-57-8
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别:
抑制剂
货号:
T3299

Product Introduction

Bioactivity

NameXevinapant hydrochloride
DescriptionXevinapant hydrochloride (AT-406 HCl) , an orally active antagonist of multiple inhibitor of apoptosis proteins(IAP), inhibits progression of human ovarian Y binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide.
Cell ResearchCells are seeded in 96-well flat bottom cell culture plates at a density of (3-4) × 103 cells/well with AT-406 and incubated for 4 days. The rate of cell growth inhibition after treatment with different concentrations of AT-406 is determined by assaying with (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-8). WST-8 is added to each well to a final concentration of 10%, and then the plates are incubated at 37 °C for 2−3 hours. The absorbance of the samples is measured at 450 nm using a TECAN ULTRA reader. Concentration of AT-406 that inhibited cell growth by 50% (IC50) is calculated by comparing absorbance in the untreated cells and the cells treated with AT-406. (Only for Reference)
Kinase AssayFluorescence Polarization Based Assays for XIAP, cIAP1, and cIAP2 BIR3 Proteins: FL-AT-406 (the fluorescently tagged AT-406) is employed to develop a set of new FP assays for determination of the binding affinities of Smac mimetics to XIAP, cIAP-1, and cIAP-2 BIR3 proteins. The Kd value of FL-AT-406 to each IAP protein is determined by titration experiments using a fixed concentration of FL-AT-406 and different concentrations of the protein up to full saturation. Fluorescence polarization values are measured using an Infinite M-1000 plate reader in Microfluor 2 96-well, black, round-bottom plates. To each well, FL-AT-406 (2, 1, and 1 nM for experiments with XIAP BIR3, cIAP-1 BIR3, and cIAP-2 BIR3, respectively) and different concentrations of the protein are added to a final volume of 125 μL in the assay buffer (100 mM potassium phosphate, pH 7.5, 100 μg/mL bovine γ-globulin, 0.02% sodium azide, with 4% DMSO). Plates are mixed and incubated at room temperature for 2-3 hours with gentle shaking. The polarization values in millipolarization units (mP) are measured at an excitation wavelength of 485 nm and an emission wavelength of 530 nm. Equilibrium dissociation constants (Kd) are then calculated by fitting the sigmoidal dose-dependent FP increases as a function of protein concentrations using Graphpad Prism 5.0 software. In competitive binding experiments for XIAP3 BIR3, AT-406 is incubated with 20 nM XIAP BIR3 protein and 2 nM FL-AT-406 in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/mL bovine γ-globulin; 0.02% sodium azide). In competitive binding experiments for cIAP1 BIR3 protein, 3 nM protein and 1 nM FL-AT-406 are used. In competitive binding experiments for cIAP2 BIR3, 5 nM protein and 1 nM FL-AT-406 are used. For each competitive binding experiment, polarization values are measured after 2-3 hours of incubation using an Infinite M-1000 plate reader.The IC50 value, the inhibitor concentration at which 50% of the bound tracer is displaced, is determined from the plot using nonlinear least-squares analysis. Curve fitting is performed using the PRISM software. A Ki value for AT-406 is calculated.
In vitroAT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. AT-406 is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. AT-406 (at 1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, AT-406 induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. AT-406 effectively inhibits lots of human cancer cell lines and shows IC50 of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. AT-406 induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP. [1]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 100 mg/mL (178.02 mM)
Ethanol : 100 mg/mL (178.02 mM)
H2O : <1 mg/mL
Keywordsdegradation | Xevinapant Hydrochloride | mimetic | AT-406 | ovarian | oral | Xevinapant hydrochloride | IAP | AT406 | cancer | Debio-1143 | Debio1143 | SM 406 | Debio 1143 | Xevinapant | Smac | SM406 | Inhibitor | inhibit | AT 406
Inhibitors RelatedLidocaine hydrochloride | Metronidazole | 5-Fluorouracil | Stavudine | Tributyrin | Dextran sulfate sodium salt (MW 4500-5500) | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Sodium 4-phenylbutyrate | Kaempferol
SM-406|||AT-406 HCl|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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