MS436 - CAS:1395084-25-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	MS436
英文名称:	MS436
别名:	MS436 MS-436; (E)-4-[2-(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-2-pyridinylbenzenesulfonamide
CAS No:	1395084-25-9	分子式:	C₁₈H₁₇N₅O₃S	分子量:	383.43
CAS No:	1395084-25-9
分子式:	C₁₈H₁₇N₅O₃S
分子量:	383.43

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M10321 MS436 ≥98%(HPLC) (psaitong)

相关产品

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(25mg/mL 超声加热)

产品描述：

基本信息

产品编号：M10321
产品名称：MS436
CAS:	1395084-25-9	储存条件	粉末	-20℃	四年

分子式：	C18H17N5O3S		溶于液体	-80℃	六个月
分子量：	383.43			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	55mg/mL (143.44mM)
		Ethanol	1mg/mL warmed with 50ºC water bath (2.6mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.6081mL	13.0405mL	26.0811mL
5mM	0.5216mL	2.6081mL	5.2162mL
10mM	0.2608mL	1.3041mL	2.6081mL
50mM	0.0522mL	0.2608mL	0.5216mL

生物活性

产品描述	一种BRD4抑制剂。
靶点/IC50	BRD4 (1)	BRD4 (2)
	<0.085μM(Ki)	0.34μM(Ki)
体外研究	MS436,through a set of water-mediated interactions,exhibits low nanomolar affinity (estimated Ki of 30-50nM) with preference for the first bromodomain over the second.MS436 effectively inhibits BRD4 activity in NF-κB-directed production of NO and pro-inflammatory cytokine interleukin-6 in murine macrophages.MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.MS436 exhibits potent affinity of an estimated Ki=30-50nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2,which is achieved through a unique set of water-mediated intermolecular interactions.

推荐实验方法(仅供参考)

激酶实验：

Binding affinity of the newly synthesized diazobenzene compounds (e.g.,MS436) for various bromodoamins is assessed in a fluorescence anisotropy competition assay using a fluorescein isothiocyanate (FITC)-labeled MS417 as an assay probe.Competition experiments are performed with a BrD protein (0.25-1µM) and the fluorescent probe (80nM),and increasing concentration of unlabeled competing ligand in a PBS buffer (pH 7.4) in total volume of 80µL Measurements are obtained after a 1 hour incubation of the fluorescent ligand and the protein at 25℃ with Safire 2 microplate reader.In a competitionbinding assay,fluorescent ligand concentration is≤2Kd,and protein concentration is set at which 50-80% of fluorescent ligand is bound.Dissociation constant of a competing ligand is calculated with the correction to Cheng-Prussoff equation introduced by Nicolovska-Coleska and colleagues.Assuming one-site competitive binding model,the equation used to calculate Ki’s from IC50 values.

细胞实验:

Murine macrophage RAW264.7 cells are plated at a density of 1×104 cells per well in a 96-well plate and incubated at 37℃ for 18h.The cells are then treated with the diazobenzene bromodomain inhibitors (e.g.,MS436) up to 100µM for 24 hours.At the end of the 24hr incubation,10µL of the MTT solution (4mg/mL) is added to each well and incubated at 37℃ for 4h.The supernatants are then removed and the cells are solubilized in 100µL of 100% DMSO.The diazobenzene compounds are first dissolved in DMSO then diluted with culture medium to concentrations that ranged from 0.28 to 50000nM.The final concentration of DMSO is adjusted to 0.05% (v/v).The extent of the reduction is measured by the absorbance at 570/630nm using EnVison 2104 Multilabel Reader

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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