DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
IC50&Target
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)
体外研究
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. DMAT has effects on H295R cell proliferation at concentrations of 10 and 10mol/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. 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.
体内研究
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.
分子式
C9H7Br4N3
分子量
476.79
CAS号
749234-11-5
运输条件
Room temperature in continental US; may vary elsewhere.