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DMAT  ≥98%

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包装规格：10mg 50mg 100mg 1g in glass bottle
溶解性：溶于DMSO（50 mg/mL 超声）
产品描述：基本信息 产品编号：D10800 产品名称：DMAT CAS: 749234-11-5   储存条件 粉末 -20℃ 四年     分子式： C9H7Br4N3 溶于液体 -80℃ 六个月 分子量 476.79 -20℃ 一个月 化学名：  4,5,6,7-TETRABROMO-N,N-DIMETHYL-1H-BENZIMIDAZOL-2-AMINE   Solubility (25°C)   体外 DMSO 50mg/mL (104.87mM; Need ultrasonic) Ethanol   Water   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 2.0974mL 10.4868mL 20.9736mL 5mM 0.4195mL 2.0974mL 4.1947mL 10mM 0.2097mL 1.0487mL 2.0974mL   生物活性 产品描述 一种有效的，特异性的 CK2 抑制剂，IC50 值为 130nM。 靶点/IC50 CK2 0.13μM (IC50, Human CK2) PIM1 0.148μM (IC50) PIM2 1.6μM (IC50) PIM3 0.097μM (IC50) HIPK2 0.37μM (IC50) HIPK3 0.59μM (IC50) DYRK1a 0.41μM (IC50) DYRK2 0.35μM (IC50) DYRK3 1.7μM (IC50) PKD1 0.18μM (IC50) CDK2 0.64μM (IC50)   体外研究 DMAT (1 μM-2.5μM) DMAT is more efficient in killing antiestrogen resistant cells than parental antiestrogen sensitive MCF-7 cells. DMAT-induced cell death of antiestrogen resistant cells is mediated by caspases. DMAT inhibits CK2 activity but the inhibition is similar in the three cell lines, MCF-7, TAMR-1 and 182R-6. DMAT has effects on H295R cell proliferation at concentrations of 10-4 and 10-5mol/Las compared with the control. DMAT (100μM) significantly increases apoptosis of H295R cells. DMAT (1 nM-1μM) significantly decreases aldosterone release into supernatants of 72-h H295R cell cultures as compared with the control. DMAT also inhibits PIM1 by a mechanism which is competitive with respect to ATP, and it is a powerful inhibitor of kinases other than CK2 体内研究 DMAT application in vivo reduces tumor growth in a xenotransplant model by interference with tumor cell proliferation. Biochemical parameters and histology following DMAT administration revealed no alterations in liver tissue.   推荐实验方法(仅供参考) 激酶实验： Kinase Assay Kinase activity tests are performed in a volume of 50μL containing (final concentrations): 0.1μg/μL protein extract, 500μM CK2 substrate peptide (RRRDDDSDDD), 25mM Tris-HCl, pH 8.5, 100μM Na3VO4, 1mM DTT, 20mM NaCl, 5mM MgCl2, 50μM ATP and appr 1μCi [γ-32P]-ATP (3000 Ci/mmol). Samples are incubated for 10 min at 30°C. Aliquots are spotted onto P81 phosphocellulose paper and washed 3×5 min in 0.75% phosphoric acid and once in acetone. Incorporation of radiolabelled phosphate is measured by counting the samples in a liquid scintillation counter. Three independent experiments, each done in duplicate, are performed with reproducible results.   细胞实验:   Cell Assay H295R cells are plated at a density of 2×104  cells/well into 96-well microplates in complete culture medium and preincubated for 12 h (5% CO2, 37°C, 95% humidity). DMAT in 96% ethanol and Nu-Serum-free culture medium is added to the appropriate wells at final concentrations of 10-4-10-10 M (the highest concentration of ethanol is 1.8% [vol] in the 10-4 M wells). The same volume of Nu-Serum-free culture medium and 96% ethanol is added to the control wells at the same concentration as the solvent in the 10-4 M group. Incubation is performed for 72 h under standard conditions (5% CO2, 37°C,95% humidity). The absorbance (OD, optical density) of each sample is measured with an enzyme-linked immunosorbent assay (ELISA) microplate reader at a wavelength of 450nm
保存条件：-20℃

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