UNC669是一种有效且特异性的 MBT（恶性脑瘤）抑制剂，是甲基赖氨酸结合结构域的配体，是L3MBTL1和L3MBTL3的抑制剂，IC50分别为 4.2 和 3.1 uM。

UNC669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.

In vitro Enzyme Assays.: All in vitro enzyme assays are done at Upstate Biotechnology with the exception of InsR and IGF-1R. To determine the IC50 of TAE684 against InsR and IGF-1R a homogeneous time-resolved fluorescence assay is performed. ATP (10 mM) and 20 mg/ml biotinylated PolyEY (Glu, Tyr 4:1) are combined with 50 nL of serial dilutions of TAE684 (10-500 nM) and 4 ng of InsR enzyme in the presence of the kinase reaction buffer (20 mM Tris譎Cl, pH 7.5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA). Assays are incubated for 1 hour at ambient temperature. Reactions are terminated by adding 10 mL of the detection solution containing 50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/mL Eu3+ cryptate-labeled anti-phosphotyrosine antibody Mab PT66-K, and 5 mg/mL Streptavidin-XLent. The reaction is incubated for half an hour, and fluorescence signals are read on Analyst GT.

1314241-44-5

C15H20BrN3O

338.24

UNC669;UNC 669

Ethanol:63 mg/mL (186.3 mM)
H2O:<1 mgml
DMSO:9 mg/mL (26.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years