DMAT

DMAT

Application

DMAT has been used as a casein kinase 2 (CK2) inhibitor:to study its effects on parasite multiplication in a [3H]-hypoxanthine incorporation assayto study its effects on the intracellular response in prostate cancer cellsto study its effects on cell division cycle 25C (cdc25C) phosphatase levels in prostate cancer cells

Biochem/physiol Actions

DMAT is an ATP-competitive (Ki = 40 nM) casein kinase 2 (CK2) inhibitor (IC50 = 140 nM; rat liver CK2, [ATP] = 20 nM) with greatly improved potency and selectivity than its structure analog TBB. With the exception of DYRK1a (IC50 = 120 nM), DMAT is reported to exhibit no CK1 inhibitiory potency up to 200 µM (50% inhibition by 29 µM TBB) and little or no activity against a panel of 32 other protein kinases, nor PI3K α and γ. When tested in Jurkat cultures, DMAT is shown to be a superior apoptosis inducer than TBB (DC50 = 2.7 µM/DMAT vs. 17 µM/TBB).

Casein kinase II inhibitor II (Ck2 Inhibitor II) is a high affinity ATP-competitive inhibitor of casein kinase II. Ck2 Inhibitor II inhibits CK2 in rat liver with 1,300-fold greater selectivity for CK2 than for CK1 (IC50 = 140 nM and >200 µM respectively). Ki = 40 nM; In Jurkat human T-cell leukemia cells, Ck2 Inhibitor II does not display side effects on mitochondria polarization at concentrations up to 10 µM; Ck2 Inhibitor II is useful for in vivo studies due to cell permeability and high efficacy in cultured cells and has implications in research and treatment of neoplasia and infective diseases, in which CK2 plays a role and is highly active constitutively.

Caution

Air sensitive

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Code Description Colour Manufacturer Storage Temp. Form Assay Price Quantity
3575740 DMAT white to beige SIGMA-ALDRICH −20°C powder ≥98% (HPLC)
£344.04 (exc VAT) per 25MG
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3575741 DMAT white to beige SIGMA-ALDRICH −20°C powder ≥98% (HPLC)
£106.28 (exc VAT) per 5MG
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