DMAT|749234-11-5|(CK2 Inhibitor; Casein kinase II Inhibitor)-陌孚医药/Medlife

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DMAT (Synonyms: CK2 Inhibitor; Casein kinase II Inhibitor)

目录号: PC15433 纯度: ≥98%

CAS No. :749234-11-5

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PC15433-50mg	50mg	¥2812.60	请登录
PC15433-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥862.40	请登录

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中文名称

DMAT

中文别名

2-二甲基氨基-4,5,6,7-四溴苯并咪唑

英文名称

4,5,6,7-Tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine

英文别名

4,5,6,7-tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine;1H-Benzimidazol-2-amine, 4,5,6,7-tetrabromo-N,N-dimethyl-;DMAT;Casein kinase II Inhibitor;CK2 Inhibitor;2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole;4,5,6,7-Tetrabromo-N,N-dimethyl-1H-benzo[d]imidazol-2-amine;CK2 Inhibitor II;ck2inhibitor;CK2 Inhibitor II, DMAT;DIMETHYL-(4,5,6,7-TETRABROMO-1H-BENZOIMIDAZOL-2-YL)-AMINE;Casein Kinase II Inhibitor II, DMAT;InSolution™ Casein Kinase II Inhibitor, DMAT;1zoe;K25;CK2 Inhibitor 2;DMAT(CK2 Inhibitor);C9H7br4N3;GTPL9323

Cas No.

749234-11-5

分子式

C₉N₃Br₄H₇

分子量

476.79

包装储存

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

生物活性

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

性状

Solid

IC50 & Target[1][2]

CK2

0.13 μM (IC₅₀, Human CK2)

PIM1

0.148 μM (IC₅₀)

PIM2

1.6 μM (IC₅₀)

PIM3

0.097 μM (IC₅₀)

HIPK2

0.37 μM (IC₅₀)

HIPK3

0.59 μM (IC₅₀)

DYRK1a

0.41 μM (IC₅₀)

DYRK2

0.35 μM (IC₅₀)

DYRK3

1.7 μM (IC₅₀)

PKD1

0.18 μM (IC₅₀)

CDK2

0.64 μM (IC₅₀)

体外研究(In Vitro)

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. DMAT has effects on H295R cell proliferation at concentrations of 10 and 10mol/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. 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.

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

体内研究(In Vivo)

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

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

参考文献

[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. [Information]

[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) 体外研究. Cell Tissue Res. 2010 May;340( [Information]

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

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0974 mL	10.4868 mL	20.9736 mL
5 mM	0.4195 mL	2.0974 mL	4.1947 mL
10 mM	0.2097 mL	1.0487 mL	2.0974 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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