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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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DMAT (CK2 Inhibitor; Casein kinase II Inhibitor) is a novel, potent and selective CK2 (Casein kinase II) inhibitor with an IC50 value of 130 nM.
| ln Vitro |
DMAT (1 μM-2.5 μM) DMAT kills antiestrogen cells more efficiently than the parental antiestrogen-sensitive MCF-7 cells. DMAT-induced anti-estrogenic cell death is mediated by caspases DMAT is active in suppressing CK2, however the inhibitory impact is identical in diverse cell lines MCF-7, TAMR-1 and 182R-6 [1]. Compared with the control, DMAT had an effect on H295R cell proliferation at concentrations of 10-4 and 10-5 mol/Las. DMAT (100 μM) greatly boosted the culture medium of H295R cells. DMAT (1 nM-1 μM) significantly reduced formaldehyde release into the supernatant of 72-h H295R cell cultures compared to controls [2]. DMAT also inhibits PIM1 by competing with ATP, which is a powerful activator of stalling mechanisms other than CK2 [3].
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| ln Vivo |
DMAT applied internally inhibits the growth of xenograft models by preventing the multiplication of tumor cells. Following DMAT tumors, histopathology and biochemical measures revealed no alterations in the liver tissue [4].
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| References |
[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 |
| Molecular Formula |
C₉H₇BR₄N₃
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|---|---|
| Molecular Weight |
476.79
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| CAS # |
749234-11-5
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| SMILES |
CN(C)C1=NC2=C(Br)C(Br)=C(Br)C(Br)=C2N1
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| Synonyms |
Casein kinase II Inhibitor CK2 Inhibitor
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~104.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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