K03861
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.
K03861是CDK2的II型抑制剂。细胞周期蛋白依赖性激酶全酶包含一个催化亚基CDK、一个可调节亚基以及细胞周期蛋白。CDKs是哺乳动物异源二聚体丝氨酸/苏氨酸激酶的催化亚基,细胞周期蛋白依赖性激酶(CDKs)在细胞周期调节、转录和神经元功能中起着重要作用。在某些人类肿瘤中,CDK下调。靶向CDK的抑制剂被认为可以调节cyclin-CDK复合物,阻止细胞增殖。CDK在细胞周期调控中的中心作用使它们成为研究改变细胞增殖的抑制剂分子的重要靶标[1]。
K03861是CDK2的氨基嘧啶苯脲类抑制剂。CDK2与II型抑制剂K03861共结晶结构揭示了典型的II型抑制剂结合模式。II型抑制剂可以与细胞周期蛋白结合相对抗。II型抑制剂结合的重要氨基酸可能与ATP结合口袋距离较远。这种复合物的晶体结构为研究细胞周期蛋白竞争性CDK2抑制剂提供了重要的结构基础[2]。
参考文献:
Malumbres M, Barbacid M. Mammalian cyclin-dependent kinases[J]. Trends in biochemical sciences, 2005, 30(11): 630-641.
Alexander L T, Mobitz H, Drueckes P, et al. Type II inhibitors targeting CDK2[J]. ACS chemical biology, 2015, 10(9): 2116-2125.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 501.5 |
Cas No. | 853299-07-7 |
Formula | C24H26F3N7O2 |
Solubility | ≥50.2 mg/mL in DMSO; insoluble in H2O; ≥45.4 mg/mL in EtOH |
Chemical Name | 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC(N)=NC=C4)C=C3)=O)C=C2)CC1 |
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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