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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PIKfyve-RMC-113
RMC-113

Chemical Structure : RMC-113

CAS No.: 2258606-34-5

RMC-113 (RMC113)

货号: PC-22226Not For Human Use, Lab Use Only.

RMC-113 a potent small molecule dual inhibitor of lipid kinases PIP4K2C and PIKfyve with binding Kd of 370 nM and 46 nM respectively, potently suppresses the replication of multiple RNA viruses including SARS-CoV-2.

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    生物&药学活性

    RMC-113 a potent small molecule dual inhibitor of lipid kinases PIP4K2C and PIKfyve with binding Kd of 370 nM and 46 nM respectively, potently suppresses the replication of multiple RNA viruses including SARS-CoV-2.
    RMC-113 suppresses the enzymatic activity of PIKfyve (IC50=8 nM).
    RMC-113 shows IC50 of 392 nM and 299.8 nM for PIP4K2C and PIKfyve in cell-based target engagement analysis via live-cell NanoBRET assays.
    RMC-113 displays no activity against PIP4K2A and PIP4K2B, and low or no affinity for other kinases and overall excellent selectivity against 335 kinase panel.
    RMC-113 dose dependently inhibits replication of WT and SARS-CoV-2 expressing Nluc-reporter (rSARS CoV-2/Nluc (USA-WA1/2020 strain)) in human lung epithelial (Calu-3) cells, as measured via plaque (EC50=0.25 μM) and luciferase (EC50=1.45 μM) assays, respectively.
    RMC-113 also suppresses replication-restricted pseudovirus bearing SARS CoV-2 spike (S) protein (rVSV-SARS-CoV-2-S) in Vero cells (EC50=1.8 μM).
    RMC-113 dose-dependently suppressed SARS-CoV-2 replication measured in ALO culture supernatants by plaque assays (EC50=0.15 μM) and nucleocapsid (N) transcript expression measured in ALO lysates by RT-qPCR (EC50=0.35 μM), and CC50 >10 μM.

    物理化学性质&存储条件

    分子量 373.43
    分子式 C21H15N3O2S
    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

    6-(3,4-dimethoxyphenyl)-3-(pyridin-3-ylethynyl)isothiazolo[4,3-b]pyridine

    参考文献

    1. Marwah Karim, et al. bioRxiv. 2024 Apr 17:2024.04.15.589676.

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