PD318088
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.
PD318088是MEK1/2的非ATP竞争性的变构抑制剂。
PD318088是PD184352的类似物，这意味着它可能具有针对癌细胞的抗增殖活性，但是目前没有关于PD318088的功能研究。PD318088与ATP同时结合于MEK1的活性部位，其与ATP结合位点是相邻的。MEK1和MEK2的单体或二聚体与PD318088和MgATP形成的三元复合物导致Kd值适度增加，达到140 nM。PD318088和MgATP增加MEK1和MEK2二聚体的解离常数，从大约75 nM增加到大约140 nM[1]。
PD318088是一个芳基胺化合物，可与MEK共结晶。G8935占据毗邻ATP结合位点的特定口袋，并与PD318088结合位点重叠。PD318088可与Ile216、Phe209、Arg189和Asp190形成的结合口袋相结合[2]。
参考文献：
1. Ohren JF1, Chen H, Pavlovsky A et al. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. Epub 2004 Nov 14.
2. Han S, Zhou V, Pan S et al. Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5467-73. Epub 2005 Sep 30.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 561.09 |
| Cas No. | 391210-00-7 |
| Formula | C16H13BrF3IN2O4 |
| Solubility | ≥28.05 mg/mL in DMSO; insoluble in H2O; ≥7.36 mg/mL in EtOH with ultrasonic |
| Chemical Name | 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C=C1I)F)NC2=C(C(=C(C=C2C(=O)NOCC(CO)O)Br)F)F |
| 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。 |
| Description | PD 318088是MEK1/2的非ATP竞争性的变构抑制剂。 | |||||
| 靶点 | MEK1/2 | |||||
| IC50 | ||||||
化学结构
