| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
DMAT targets casein kinase 2 (CK2), a serine/threonine kinase involved in various cellular processes including cell proliferation, apoptosis, and DNA repair. It is an ATP-competitive inhibitor with an IC50 of 130 nM for CK2. It also inhibits Pim-1, Pim-3, HIPK2, and HIPK3.
|
|---|---|
| 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].
In vitro, DMAT is a potent and specific CK2 inhibitor with an IC50 of 130 nM. It inhibits CK2 in rat liver with 1,300-fold greater selectivity for CK2 than for CK1 (IC50 = 140 nM and >200 μM, respectively). It also inhibits Pim-1, Pim-3, HIPK2, and HIPK3 with IC50 values of 150 nM, 97 nM, 370 nM, and 590 nM, respectively. |
| 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].
In vivo activity data for DMAT are limited. As a CK2 inhibitor, it would be expected to modulate CK2-dependent signaling pathways in vivo, potentially affecting cell proliferation, apoptosis, and inflammation. Further in vivo studies are needed to confirm its efficacy and establish pharmacokinetic profiles. |
| Enzyme Assay |
In vitro kinase inhibition assays for DMAT are conducted using purified recombinant CK2, Pim-1, Pim-3, HIPK2, and HIPK3 kinases. Kinase activity is measured using radiolabeled ATP (³³P-ATP) or fluorescence-based assays such as time-resolved fluorescence resonance energy transfer (TR-FRET). The compound is incubated with the kinase, substrate, and ATP at varying concentrations, and IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cellular assays for DMAT are performed using cancer cell lines or other relevant cell types. Cells are treated with compound concentrations ranging from 0.01 to 100 µM for 24-72 hours. CK2 activity is measured by assessing the phosphorylation of CK2 substrates (e.g., Akt, p53) via Western blotting. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated by flow cytometry.
|
| Animal Protocol |
In vivo animal studies for DMAT would typically utilize tumor xenograft models or models of diseases where CK2 is dysregulated. The compound is administered orally or intraperitoneally. Endpoints include tumor growth, CK2 activity in tissues, and biomarkers of CK2 signaling.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of DMAT are not well characterized. The compound has a molecular weight of 476.79 and a molecular formula of C₉H₇Br₄N₃. It is cell-permeable, suggesting it can cross cell membranes. Standard PK studies in rodents would be required.
|
| Toxicity/Toxicokinetics |
Toxicological data for DMAT are limited. As a research compound, it is designated for laboratory use only. No significant acute toxicity has been reported. Standard toxicity screening would involve acute and repeated-dose studies in rodents.
|
| References |
|
| Additional Infomation |
DMAT is a potent and specific CK2 inhibitor (IC50 = 130 nM). It has 1,300-fold selectivity for CK2 over CK1 and also inhibits Pim-1, Pim-3, HIPK2, and HIPK3. It has a molecular weight of 476.79 and formula C₉H₇Br₄N₃. It is not clinically approved.
|
| Molecular Formula |
C₉H₇BR₄N₃
|
|---|---|
| Molecular Weight |
476.79
|
| Exact Mass |
472.737
|
| CAS # |
749234-11-5
|
| PubChem CID |
5326976
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.678
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
16
|
| Complexity |
265
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SLPJGDQJLTYWCI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H7Br4N3/c1-16(2)9-14-7-5(12)3(10)4(11)6(13)8(7)15-9/h1-2H3,(H,14,15)
|
| Chemical Name |
4,5,6,7-tetrabromo-N,N-dimethyl-1H-benzimidazol-2-amine
|
| Synonyms |
Casein kinase II Inhibitor CK2 Inhibitor
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~104.87 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
