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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-SCR-6920
SCR-6920

Chemical Structure : SCR-6920

CAS No.: 2756849-68-8

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SCR-6920 (SCR6920)

货号: PC-26595Not For Human Use, Lab Use Only.

SCR-6920 is a potent and selective, oral PRMT5 inhibitor with IC50 of 1.48 nM.

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

    生物&药学活性

    SCR-6920 is a potent and selective, oral PRMT5 inhibitor with IC50 of 1.48 nM.
    SCR-6920 binds to substrate pocket, adjacent to the binding site of the cofactor SAM, does not affect the binding of MEP50 to PRMT5.
    SCR-6920 shows no inhibitory activity against other TRPM family members such as PRMT1, PRMT3, PRMT6, and PRMT8 (IC50>50 uM).
    SCR-6920 demonstrates broad antitumor activities on a range of tumors with IC50 of <600 nM for 15 out of 25 for lung cancer, 5 out of 6 for ovarian cancer, 9 out of 14 for breast cancer, 3 out of 3 for head and neck cancer, 3 out of 4 for bladder cancer, and 4 out of 4 for lymphoma.
    SCR-6920 has IC50 values of 17.5 nmol/L (A375), 7.4 nmol/L (A549), 10.4 nmol/L (MDA-MB-468), 8.4 nmol/L (5637), 3.42 nmol/L (Z138), and 15.6 nmol/L (Raji), with minimal cytotoxicity to nonmalignant cell lines.
    SCR-6920 regulates transcription profiles associated with DNA damage and angiogenesis in ovarian cancer.
    SCR-6920 downregulates hypoxia-inducible factor-1α (HIF-1α) through the ubiquitin–proteasome degradation pathway, thereby reducing downstream VEGF expression and secretion.
    SCR-6920 demonstrates a synergistic effect for SCR-6920 combined with bevacizumab against ovarian cancer.

    物理化学性质&存储条件

    分子量 546.71
    分子式 C32H42N4O4
    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

    1-ethyl-4-((R)-2-hydroxy-2-((S)-1,2,3,4-tetrahydroisoquinolin-3-yl)ethyl)-8-(2-methoxy-7-azaspiro[3.5]nonane-7-carbonyl)-1,2,3,4-tetrahydro-5H-benzo[e][1,4]diazepin-5-one

    参考文献

    1. Yang G, et al. Mol Cancer Ther. 2026 Apr 21. doi: 10.1158/1535-7163.MCT-25-1105.

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