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.
NVP-LCQ195
目录号: GC16959纯度: >99.50%同义词: 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
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
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥388.00 | 现货 | 1 | |
| 5mg | ¥900.00 | 现货 | 1 | |
| 10mg | ¥1,372.00 | 现货 | 1 | |
| 25mg | ¥2,560.00 | 现货 | 1 | |
| 50mg | ¥3,640.00 | 现货 | 1 | |
| 100mg | ¥5,098.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥912.00 | 现货 | 1 |
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产品描述 Description
产品文档 Product Documents
Purity:>99.50%
化学性质Chemical Properties
CAS 号
902156-99-4
同义词
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
SMILES
CS(=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 g/mol
溶解性
≥ 152.4 mg/mL in DMSO, ≥ 3.28 mg/mL in EtOH with ultrasonic and warming
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。
计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度
g/mol