DMAT is a potent and specific CK2 inhibitor with an IC₅₀ value of 130 nM.

DMAT (1 μM-2.5 μM) 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^[1]. DMAT has effects on H295R cell proliferation at concentrations of 10^-4 and 10^-5mol/Las compared with the control. DMAT (100 μM) significantly increases apoptosis of H295R cells. DMAT (1 nM-1 μM) significantly decreases aldosterone release into supernatants of 72-h H295R cell cultures as compared with the control^[2]. 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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

476.79

C₉H₇Br₄N₃

749234-11-5

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (104.87 mM; Need ultrasonic)

*

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Yde CW, et al. Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitorDMAT. Cancer Lett. 2007 Oct 28;256(2):229-37.

  [2]. Lawnicka H, et al. Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro. Cell Tissue Res. 2010 May;340(

  [3]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65.

  [4]. Sass G, et al. Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT. Int J Oncol. 2011 Aug;39(2):433-42.

Kinase activity tests are performed in a volume of 50 μL containing (final concentrations): 0.1 μg/μL protein extract, 500 μM CK2 substrate peptide (RRRDDDSDDD), 25 mM Tris-HCl, pH 8.5, 100 μM Na₃VO₄, 1 mM DTT, 20 mM NaCl, 5 mM MgCl₂, 50 μM ATP and appr 1 μCi [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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 450 nm.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Yde CW, et al. Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitorDMAT. Cancer Lett. 2007 Oct 28;256(2):229-37.

  [2]. Lawnicka H, et al. Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro. Cell Tissue Res. 2010 May;340(

  [3]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65.

  [4]. Sass G, et al. Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT. Int J Oncol. 2011 Aug;39(2):433-42.