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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Hexokinase-Tuvatexib
Tuvatexib

Chemical Structure : Tuvatexib

CAS No.: 2055404-90-3

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Tuvatexib (Hexokinase 2 modulator Comp-1)

货号: PC-35768Not For Human Use, Lab Use Only.

Tuvatexib (Hexokinase 2 modulator Comp-1) is a potent, selective small molecule modulator of Hexokinase 2 (HK2) interaction with the mitochondria, selectively dissociates HK2 from VDAC1 in vitro with IC50 of 92 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Tuvatexib (Hexokinase 2 modulator Comp-1) is a potent, selective small molecule modulator of Hexokinase 2 (HK2) interaction with the mitochondria, selectively dissociates HK2 from VDAC1 in vitro with IC50 of 92 nM.
    Tuvatexib does not affect the VDAC1/HK1 complex.
    Tuvatexib dose-dependent reduces mitochondrial-bound HK2 levels in human skin SCC A431 cells with IC50 of 0.8 uM, reduces glycolysis and triggers apoptosis in cancer cells, without affecting hexokinase 1-expressing normal cells.
    Tuvatexib demonstrates anti-cancer activity in UVB-damaged skin model in SKH-1 mice.

    物理化学性质&存储条件

    分子量 337.419
    分子式 C21H23NO3
    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

    Quinolin-8-yl (Z)-2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate

    参考文献

    1. Behar V, et al. J Invest Dermatol. 2018 Jun 14. pii: S0022-202X(18)32056-6.

    2. Goldin N, et al. Oncogene. 2008 Aug 7;27(34):4636-43.

    3. Krasnov GS, et al. Expert Opin Ther Targets. 2013 Oct;17(10):1221-33.

    4. PCT Int. Appl. (2018), WO 2018083705 A1 20180511.

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