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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
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
NVP-LCQ195 (AT9311; LCQ195) 是 CDK1、CDK2、CDK3 和 CDK5 的小分子杂环抑制剂,IC50 为 1-42 nM。
Cas No.902156-99-4
别名4-(2,6-二氯苯甲酰基氨基)-1H-吡唑-3-羧酸N-[1-(甲基磺酰基)哌啶-4-基]酰胺,LCQ-195;AT-9311;NVP LCQ195;LCQ 195;AT9311;AT 9311
化学名4-[(2,6-dichlorobenzoyl)amino]-N-(1-methylsulfonylpiperidin-4-yl)-1H-pyrazole-5-carboxamide
Canonical SMILESCS(=O)(=O)N1CCC(CC1)NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl
分子式C17H19Cl2N5O4S
分子量460.33
溶解度≥ 152.4 mg/mL in DMSO, ≥ 3.28 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.