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NVP-LCQ195
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NVP-LCQ195图片
CAS NO:902156-99-4
规格:98%
分子量:460.33
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
CDK1/CDK2/CDK5 inhibitor
CAS:902156-99-4
分子式:C17H19Cl2N5O4S
分子量:460.33
纯度:98%
存储:Store at -20°C

Background:

NVP-LCQ195 is a pan-inhibitor of CDKs [1].
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 [1].
In bortezomib-treated MM patients, NVP-LCQ195 suppressed high expression of genes and significantly increased progression-free and overall survival [1].
Reference:
[1]. 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.