1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  2. Casein Kinase

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

Cat. No.: HY-15535 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

DMAT Chemical Structure

DMAT Chemical Structure

CAS No. : 749234-11-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 343 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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View All Casein Kinase Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[3]

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)

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[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].

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[4].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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.

Cell Assay
[2]

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.

References
Molecular Weight

476.79

Formula

C₉H₇Br₄N₃

CAS No.

749234-11-5

SMILES

CN(C)C1=NC2=C(Br)C(Br)=C(Br)C(Br)=C2N1

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

Room temperature in continental US; may vary elsewhere

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DMAT
Cat. No.:
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DMAT

Cat. No.: HY-15535