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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-LIM Kinase (LIMK)-MDI-114215
MDI-114215

Chemical Structure : MDI-114215

CAS No.:

MDI-114215 (MDI 114215)

货号: PC-23696Not For Human Use, Lab Use Only.

MDI-114215 is a potent, allosteric, and highly selective dual-LIMK1/2 inhibitor with IC50 of 20/27 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MDI-114215 is a potent, allosteric, and highly selective dual-LIMK1/2 inhibitor with IC50 of 20/27 nM respectively.
MDI-114215 inhibits PAK1-phosphorylated LIMK1/2 activity with pIC50 of 7.89 and 7.96, and reduces cellular p-cofilin levels in the AlphaLISA assay.
MDI-114215 does not bind TESK1, a close neighbor that is a member of the TKL kinase family, nor to CaMKIV, MRCKα, PAK1–2/4 or ROCK1/2.
MDI-114215 decreases phosphorylated cofilin levels ex vivo and reverses the deficit in LTP of mouse Fmr1 KO hippocampal CA1 pyramidal neurons.
MDI-114215 reverses hippocampal LTP deficits in a mouse model of FXS, potently decreases phosphorylated cofilin levels in iPSC-derived neurons from FXS patients.

物理化学性质&存储条件

分子量 479.60
分子式 C26H29N3O4S
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

N-(Cyclopropylmethyl)-N-[[4-(2-hydroxyethylamino)phenyl]methyl]-4-(phenylsulfamoyl)benzamide

参考文献

1. Baldwin AG, et al. J Med Chem. 2024 Dec 22. doi: 10.1021/acs.jmedchem.4c02694.

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