Roscovitine (Seliciclib,CYC202)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Roscovitine(Seliciclib,CYC202)是一种选择性的周期蛋白依赖性激酶(CDK)抑制剂,有效抑制 cdc2(cdc2/cyclin B)、cdk2(cdk2/cyclin A和cdk2/cyclin E)和cdk5(cdk5/p35),IC50值分别为0.65 μM、0.7 μM、0.7 μM和0.16 μM。CDK是必不可少的细胞周期调节子,经常参与人类肿瘤的解除管制。此外,roscovitine能够抑制细胞外调节激酶erk1和erk2,IC50值分别为34 μM和14 μM[1]。
据报道,roscovitine在微摩尔浓度时抑制细胞前期/中期过渡,抑制孕酮诱导的爪蟾卵母细胞成熟,诱导海星卵母细胞和海胆胚胎停滞在晚前期[1]。
参考文献:
[1] Meijer L, Borgne A, Mulner O, Chong JP, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36.
- 1. Daiane J.Viegasa, Terri G.Edwardsb, et al. "Virtual screening identified compounds that bind to cyclin dependent kinase 2 and prevent herpes simplex virus type 1 replication and reactivation in neurons." Antiviral Research. Available online 18 October 2019, 104621.
- 2. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID:29507054
- 3. Ruegsegger GN, Toedebusch RG, et al. "Loss of Cdk5 function in the nucleus accumbens decreases wheel running and may mediate age-related declines in voluntary physical activity." J Physiol. 2016 Jul 27. PMID:27461471
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 354.45 |
Cas No. | 186692-46-6 |
Formula | C19H26N6O |
Solubility | insoluble in H2O; ≥17.72 mg/mL in DMSO; ≥53.5 mg/mL in EtOH |
Chemical Name | (2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol |
SDF | Download SDF |
Canonical SMILES | CCC(CO)NC1=NC2=C(C(=N1)NCC3=CC=CC=C3)N=CN2C(C)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
有丝分裂海胆胚胎 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
IC50: 10 μM, 60 min |
实验结果 |
受精后60分钟添加roscovitine,研究发现,roscovitine以剂量依赖性方式将细胞阻滞在晚期前期。在roscovitine滞留卵中可以观察到较大的核,这种阻滞是完全可逆的,使用海水洗涤后,卵再次进入有丝分裂周期并发育成正常的长腕幼虫。100 μM最高浓度的roscovitme可以观察到相同的现象。 |
动物实验 [2]: | |
动物模型 |
注射A4573细胞的雄性无胸腺裸鼠 |
剂量 |
腹膜内注射,每天50 mg/kg,持续5天或两个5天系列,其间休息2天。 |
实验结果 |
Roscovitine治疗小鼠的肿瘤生长速度显著低于对照组,反映了切除后观察到的显著更小的个体肿瘤体积。相对于治疗开始时的肿瘤体积,第一个5天治疗系列完成后一天,roscovitine治疗动物的肿瘤大小仅生长了f1.25倍,而未治疗的小鼠中的肿瘤已经达到原始大小的14.5倍。这些值意味着肿瘤体积产生了11.5倍的差异。从roscovitine治疗的第1天开始计数,对照动物中的肿瘤在2天内达到原始体积的三倍,而治疗动物中的肿瘤需要10天才能达到初始体积三倍。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Meijer L, Borgne A, Mulner O, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. European Journal of Biochemistry, 1997, 243(1-2): 527-536. [2] Tirado O M, Mateo-Lozano S, Notario V. Roscovitine is an effective inducer of apoptosis of Ewing's sarcoma family tumor cells in vitro and in vivo. Cancer Research, 2005, 65(20): 9320-9327. |
描述 | Roscovitine是一种有效的Cdk2/cyclin E、Cdk7/cyclin H、Cdk5/p35和cdc/cyclin B抑制剂,IC50值分别为0.1、0.49、0.16和0.65 ?M。 | |||||
靶点 | Cdk2/cyclin E | Cdk7/cyclin H | Cdk5/p35 | cdc/cyclin B | ||
IC50 | 0.1 ?M | 0.49 ?M | 0.16 ?M | 0.65 ?M |
质量控制和MSDS
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