IC261
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.
IC50为16 μM。
IC261是一种新型CK1抑制剂。
据报道,p53靶向激酶酪蛋白激酶1δ(CK1 δ)和酪蛋白激酶1ε(CK1 ε)参与调节DNA修复和染色体分离。
体外:先前研究发现,IC261可以触发有丝分裂检查点控制。在低微摩尔浓度,IC261抑制细胞分裂,导致暂时有丝分裂停滞。具有活性p53的细胞通过阻断进入S期而停滞在分裂后G1期。含有非功能性p53的细胞具有形成8N DNA含量的分裂后复制。 DNA含量的增加伴随着大量的微核和凋亡细胞。免疫荧光图像还显示,低浓度IC261可导致中心体扩增从而引起多极有丝分裂[1]。
体内:动物研究表明,鞘内注射IC261(0.1-1 nmol)可以剂量依赖性地减少由角叉菜胶或CFA诱导的机械性异常性疼痛和热痛觉过敏。此外,IC261(1μM)的浴应用显示,仅自发兴奋性突触后电流的边际效应记录在对照组小鼠的基本胶质神经元中。然而,IC261可以降低两种炎症性疼痛模型中sEPSCs的频率[2]。
临床试验:到目前为止,IC261仍处于临床前研究阶段。
参考文献:
1]. Behrend L, et al. IC261, a specific inhibitor of the protein kinases casein kinase 1-delta and -epsilon, triggers the mitotic checkpoint and induces p53-dependent postmitotic effects. Oncogene. 2000 Nov 9;19(47):5303-5313.
[2] Kurihara T,et al. Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol Pain.2014 Mar 10;10:17.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 311.33 |
Cas No. | 186611-52-9 |
Formula | C18H17NO4 |
Solubility | ≥31.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | (E)-3-(2,4,6-trimethoxybenzylidene)indolin-2-one |
SDF | Download SDF |
Canonical SMILES | COC(C=C1OC)=CC(OC)=C1/C([H])=C2C3=CC=CC=C3NC\2=O |
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。 |
质量控制和MSDS
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