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首页-小分子抑制剂&激动剂-Others-Other Targets-TR-107
TR-107

Chemical Structure : TR-107

CAS No.: 2485052-87-5

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TR-107 (TR107)

货号: PC-49211Not For Human Use, Lab Use Only.

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.

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

    生物&药学活性

    TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.
    TR-107 dose‐dependent increases ClpP activity, inhibits breast cancer cell MDA‐MB‐231 and SUM159 growth (IC50=23 and 12 nM) in a ClpP‐dependent manner, without a significant increase in apoptosis.
    TR-107 showed significantly enhanced potency of cell growth inhibition in the MDA‐MB‐231 and SUM159 cell models compared with ONC201 and ONC206.
    TR‐107 (100 nM, 6-24 h) induces time‐ and dose‐dependent reduction of multiple mitochondrial proteins (TUFM and TFAM, aconitase (ACO2) and isocitrate dehydrogenase (IDH2), and succinate dehydrogenase A (SDHA) and complex I subunit NDUFS3).
    TR‐107 reduces mitochondrial metabolic functions and inhibits OXPHOS in MDA‐MB‐231 cells.
    TR‐107 (4-8 mg/kg, p.o.) prevents tumor growth in MDA‐MB‐231 xenograft model.

    物理化学性质&存储条件

    分子量 390.871
    分子式 C22H19ClN4O
    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

    3-((3-(4-chlorobenzyl)-4-oxo-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-6(4H)-yl)methyl)benzonitrile

    参考文献

    1. Fennell EMJ, et al. Pharmacol Res Perspect. 2022 Aug;10(4):e00993.

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