PD 198306
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.
PD 198306对MEK的IC50值为8 nM[1]。
PD198306是一种有效的、选择性的和非ATP竞争性的MAPK/ERK激酶(MEK)抑制剂。MEK能磷酸化促分裂原活化蛋白激酶(MAPK)。
体外:8 nM PD198306抑制分离的MEK。在各种物种的滑膜成纤维细胞中,30 ~ 100 nM PD198306抑制MEK活性。PD 198306高度选择性地作用于MEK,对c-Src、ERK、周期蛋白依赖性激酶以及磷脂酰肌醇3-激酶的IC50值分别为>4 uM、>1 uM、>4 uM和>10 uM[1]。
体内:在家兔中,PD198306呈剂量依赖性地显著减少磷酸化ERK1/2以及MMP-1的水平。在骨关节炎家兔模型中,PD198306可以部分地减少实验动物的某些结构变化[1]。在由Streptozocin与慢性缩窄性损伤导致的神经性疼痛模型中,PD198306呈剂量依赖性地缓解静态型痛觉超敏。在腰椎脊髓中,疼痛提升ERK1和ERK2水平,而PD198306能降低ERK1和ERK2水平,从而显示出上述抗痛觉过敏作用[2]。
临床试验:到目前为止,暂无可用的临床研究数据。
参考文献:
[1] Pelletier JP, Fernandes JC, Brunet J, Moldovan F, Schrier D, Flory C, Martel-Pelletier J. In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthritis Rheum. 2003 Jun;48(6):1582-93.
[2] Ciruela A, Dixon AK, Bramwell S, Gonzalez MI, Pinnock RD, Lee K. Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br J Pharmacol. 2003 Mar;138(5):751-6.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 476.23 |
Cas No. | 212631-61-3 |
Formula | C18H16F3IN2O2 |
Solubility | Soluble in DMSO |
Chemical Name | N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-((4-iodo-2-methylphenyl)amino)benzamide |
SDF | Download SDF |
Canonical SMILES | IC1=CC=C(C(C)=C1)NC(C(C(NOCC2CC2)=O)=CC(F)=C3F)=C3F |
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。 |