Matthew David Alexander, Joseph John McDonald, Yike Ni, Deqiang Niu, Russell C. Petter, Lixin QQiao, Juswinder Singh, Tao Wang, and Zhendong Zhu
- CELGENE AVILOMICS RESEARCH INC., Bedford, MA (US)
The present invention provides compounds, compositions thereof, and methods of using the same.
CovalX Technology Used
Target MK2 was modified with a test compound which indicated that the compound covalently bound to MK2. In order to assess the modified MK2 via mass spectrometry, an intact MK2 was first incubated for 60 minutes with an excess of compound (10 fold) to protein. 5 μL aliquots were removed from the incubated MK2 and diluted with 15 μL of 0.2% TFA. The diluted samples were pipetted onto a MALDI target with a matrix (sinapic acid (10mg/ml) in 0.1% TFA:Acetonitrile 50:50). The MALDI target was analyzed using a mass spectrometer that had been modified with a CovalX HM3 detection system. The data from the mass spectrometry analysis was used to determine the percent modification of target MK2. This was calculated by subtracting the centroid mass of the MK2 that had been treated with the compound from the centroid mass of the control MK2 and then dividing this value by the mass of the compound.