NVP-LCQ195 is a pan-inhibitor of CDKs .
Cyclin-dependent kinases (CDKs) are a family of protein kinases and play an important role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells.
In vitro kinase activity assays, NVP-LCQ195 blocks the activity of CDK1/cyclin B and CDK2/cyclin A, CDK2/cyclin E, as well as CDK5 (both CDK5 p25 and CDK5 p35) with IC50 value of 2 nM, 2 nM, 5 nM and 1 nM, respectively. Also, it inhibited CLK3 and CHEK2 (CHK2), CDK3/cyclin E, CDK9/cyclin T1, CDK7/cyclin H and CDK6/cyclin D3. In MM.1S cells, NVP-LCQ195 (2 μM) increased the percentage of cells in S and G2/M phases early, followed by an increase in sub-G1 population. Also, NVP-LCQ195 suppressed the expression of transcription factors including myc, IRF4 and XBP-1 .
In bortezomib-treated MM patients, NVP-LCQ195 suppressed high expression of genes and significantly increased progression-free and overall survival .
. McMillin DW, Delmore J, Negri J, et al. Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications. Br J Haematol, 2011, 152(4): 420-432.
|Storage||Store at -20°C|
|Synonyms||LCQ-195;AT-9311;NVP LCQ195;LCQ 195;AT9311;AT 9311|
|Solubility||≥152.4 mg/mL in DMSO, ≥3.28 mg/mL in EtOH with ultrasonic and warming, <2.49 mg/mL in H2O|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|