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首页-小分子抑制剂&激动剂-Others-Other Targets-PCC0208017
PCC0208017

Chemical Structure : PCC0208017

CAS No.: 2623158-64-3

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PCC0208017 (PCC 0208017, PCC-0208017)

货号: PC-73077Not For Human Use, Lab Use Only.

PCC0208017 is a potent, selective dual small-molecule inhibitor of MARK3 and MARK4 with IC50 of 1.8 and 2.01 nM, respectively.

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5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PCC0208017 is a potent, selective dual small-molecule inhibitor of MARK3 and MARK4 with IC50 of 1.8 and 2.01 nM, respectively.
PCC0208017 displays lower inhibitory activity against MARK1 and MARK2, with IC50 values of 31.4 and 33.7 nM respectively, with no strong inhibitory activity against 18 common oncogenic kinases.
PCC0208017 decreases the phosphorylation of Tau, suppresses the proliferation of glioma cells GL261, U87-MG and U251 cells with IC50 of 2.77, 4.02 and 4.45 uM.
PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis, suppresses cell migration and inhibits endothelial tube formation.
PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
Microtubule-affinity regulating kinases (MARKs) are novel mammalian serine/threonine kinases that phosphorylate microtubule associated proteins (MAPs), such as Tau, and regulate cell cycle progression and cytoskeletal dynamics. Four MARK isoforms have been identified in humans (MARK1, MARK2, MARK3 and MARK4) and all are highly enriched in human brain.

物理化学性质&存储条件

分子量 403.413
分子式 C19H20F3N7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N4-((1H-pyrazol-3-yl)methyl)-N2-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine

参考文献

1. Fangfang Li, et al. Acta Pharm Sin B. 2020 Feb;10(2):289-300.

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