详情描述
DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
Product information
CAS Number: 749234-11-5
Molecular Weight: 476.79
Formula: C9H7Br4N3
Synonym:
CK2 Inhibitor
Casein kinase II Inhibitor
Chemical Name: DMAT
Smiles: CN(C)C1NC2=C(N=1)C(Br)=C(Br)C(Br)=C2Br
InChiKey: SLPJGDQJLTYWCI-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (104.87 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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. 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.
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.
References:
- Yde CW, et al. Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitorDMAT. Cancer Lett. 2007 Oct 28;256(2):229-37.
- Lawnicka H, et al. Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro. Cell Tissue Res. 2010 May;340
- Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65.
- Sass G, et al. Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT. Int J Oncol. 2011 Aug;39(2):433-42.
Products are for research use only. Not for human use.