DMAT

C₉H₇Br₄N₃

476.79

MFCD08705322

DMAT has been used as a casein kinase 2 (CK2) inhibitor:

• to study its effects on parasite multiplication in a [3H]-hypoxanthine incorporation assay
• to study its effects on the intracellular response in prostate cancer cells
• to study its effects on cell division cycle 25C (cdc25C) phosphatase levels in prostate cancer cells

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). K_i = 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.
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).

Air sensitive

≥98% (HPLC)

powder

white to beige

wet ice

−20℃

CN(C)c1nc2c(Br)c(Br)c(Br)c(Br)c2[nH]1

GHS07

Warning

H315 - H319 - H335

P302 + P352 - P305 + P351 + P338

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Respiratory system

11 - Combustible Solids

WGK 3