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首页 / 抑制剂/激动剂 / 细胞周期 / PLK / Centrinone

Centrinone {[allProObj[0].p_purity_real_show]}

货号：A541635 同义名： LCR-263

Centrinone是一种选择性和可逆的 Plk4（极性蛋白激酶4）抑制剂，Plk4 是启动中心粒/中心体组装的丝氨酸-苏氨酸蛋白激酶。

Centrinone 化学结构 CAS号：1798871-30-3
Centrinone 化学结构
CAS号：1798871-30-3
Centrinone 3D分子结构
CAS号：1798871-30-3
Centrinone 化学结构 CAS号：1798871-30-3
Centrinone 3D分子结构 CAS号：1798871-30-3
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Centrinone 纯度/质量文件 产品仅供科研

货号：A541635 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 PLK1 ↓ PLK2 ↓ PLK3 ↓ PLK4 ↓ 其他靶点 纯度
HMN-214 ✔ 99%+
SBE13 HCl ++++

PLK1, IC50: 200 pM

 		98%
Onvansertib +++

PLK1, IC50: 2 nM

 		99%+
Volasertib ++++

PLK1, IC50: 0.87 nM

 		97%
GSK461364 +++

PLK1, Ki: 2.2 nM

 		99%+
MLN0905 +++

PLK1, IC50: 2 nM

 		99%+
Ro3280 ++

PLK1, IC50: 3 nM

 		99%
(E/Z)-Rigosertib sodium +

PLK1, IC50: 9 nM

 		+

PLK2, IC50: 260 nM

 		Bcr-Abl 99%+
BI 2536 ++++

PLK1, IC50: 0.83 nM

 		++

PLK2, IC50: 3.5 nM

 		+

PLK3, IC50: 9.0 nM

 		99%+
CFI-400945 ++

PLK4, IC50: 2.8 nM

 		Tie-2 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Centrinone 生物活性

描述 Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM[1].
体外研究

Centrinone (LCR-263) shows significant specificity, being over 1000 times more selective for Polo-like kinase 4 (Plk4) than for Aurora kinases A/B, and does not impact the phosphorylation of Aurora A or B substrates at doses that cause centrosome depletion. When administered to HeLa human cervical carcinoma cells, Centrinone (LCR-263) initiates a gradual decrease in the presence of centriolar and pericentriolar material markers with each cell division cycle, leading to most cells eventually lacking centrioles and centrosomes. This effect suggests Plk4's role in centriole duplication extends to differentiated cells, as seen in the reduced number of centrioles in multiciliated Xenopus epithelial cells. Centrinone (LCR-263) treatment results in the depletion of centrosomes across various vertebrate cell lines. The absence of centrosomes causes normal cells to enter an irreversible, senescence-like state during the G1 phase through a p53-dependent mechanism, which is notable for its independence from DNA damage, stress, Hippo pathway signaling, extended mitosis, or errors in chromosome segregation[1].

Centrinone 细胞实验

Cell Line
Concentration Treated Time Description References
NIH/3T3 mouse embryonic fibroblasts 100 nM depleted centrosomes Science. 2015 Jun 5;348(6239):1155-60
A375 cells 200 nM 4 days Induced centrosome overduplication Elife. 2022 Jun 27;11:e73944
RPE-1 cells 500 nM 4 days Resulted in cells containing either a single or no centrosome Elife. 2022 Jun 27;11:e73944
HCT116 cells 100 nM 4 days Observed the dynamic properties of NuMA in acentrosomal spindle poles, finding that NuMA is more static in acentrosomal spindle poles. EMBO J. 2020 Jan 15;39(2):e102378
HeLa cells 100 nM 3-5 days Induced the formation of acentrosomal spindles to study the mechanism of spindle bipolarity establishment in human somatic cells without centrosomes. EMBO J. 2020 Jan 15;39(2):e102378
HeLa cells 125 nM at least 4 days Depletion of centrosomes by inhibiting Plk4 activity to verify the effect of Centrinone on centrosome depletion Proc Natl Acad Sci U S A. 2016 Oct 25;113(43):E6590-E6599
hTERT-RPE1 immortalized retinal pigment epithelial cells (RPE1 cells) 150 nM 5 days To analyze the effect of centrosome removal in normal and cancer cells, centrinone treatment was found to block centriole duplication, leading to p53-dependent G1 arrest J Cell Biol. 2016 Jul 18;214(2):155-66
RPE-1 cells 200 nM 4 days Induced centrosome overduplication, resulting in approximately 50% of cells with supernumerary centrosomes Elife. 2022 Jun 27;11:e73944
8305c cells 0, 2, 4, 8, 16, 32 and 64 nM 72 h Centrinone decreased cell viability, induced cell apoptosis, arrested cell cycle at G2/M phase and inactivated Wnt/β-catenin signaling in a dose-dependent manner. Cancer Biol Ther. 2023 Dec 31;24(1):2223383
C643 cells 0, 2.5, 5, 10, 20, 40 and 80 nM 72 h Centrinone decreased cell viability, induced cell apoptosis, arrested cell cycle at G2/M phase and inactivated Wnt/β-catenin signaling in a dose-dependent manner. Cancer Biol Ther. 2023 Dec 31;24(1):2223383
HeLa cells 100 nM Centrinone 20 h Inhibition of Plk4 kinase activity induced irregular, non-spherical assemblies of GFP-Plk4 Nat Commun. 2019 Apr 18;10(1):1810
HeLa human cervical carcinoma cells 100 nM 7 days led to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lacked centrioles and centrosomes Science. 2015 Jun 5;348(6239):1155-60
CHP134 neuroblastoma cells 150 nM 3 cell cycles To assess the effect of TRIM37 levels on sensitivity to PLK4 inhibition. CHP134 cells with high TRIM37 expression ceased proliferation following centrinone treatment, suggesting synthetic lethality with PLK4 inhibition. Nature. 2020 Sep;585(7825):440-446
RPE1 cells 150 nM 3 cell cycles To assess the effect of PLK4 inhibition on mitosis. Following centrinone treatment, chromosome segregation fails in ~10% of cells, leading to eventual growth arrest. Nature. 2020 Sep;585(7825):440-446

Centrinone 参考文献

[1]Wong YL. et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60.

Centrinone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.58mL

0.32mL

0.16mL

7.89mL

1.58mL

0.79mL

15.78mL

3.16mL

1.58mL

Centrinone 技术信息

CAS号1798871-30-3
分子式C26H25F2N7O6S2
分子量 633.65
SMILES Code CC1=CC(NC2=NC(SC3=CC=C(S(=O)(CC4=CC=CC([N+]([O-])=O)=C4F)=O)C=C3F)=NC(N5CCOCC5)=C2OC)=NN1
MDL No. MFCD28969654
别名 LCR-263
运输蓝冰
InChI Key HHJSKDRCUMVWKF-UHFFFAOYSA-N
Pubchem ID 91801159
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 30 mg/mL(47.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Centrinone | 1798871-30-3 | LCR-263 | LCR263 | LCR 263 | PLK4 Inhibitor | Cell Cycle/DNA Damage | Polo-like Kinase (PLK) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Centrinone 纯度/质量文件 | Centrinone 亚型比较 | Centrinone 生物活性 | Centrinone 参考文献 | Centrinone 实验方案 | Centrinone 技术信息

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