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首页-抗体药物偶连体和PROTACs-PROTAC-INY-06-061
INY-06-061

Chemical Structure : INY-06-061

CAS No.: 2919963-24-7

INY-06-061 (ERK5 PROTAC degrader)

货号: PC-49380Not For Human Use, Lab Use Only.

INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).

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

    生物&药学活性

    INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).
    INY-06-061 displays a similar selectivity profile to both the parental inhibitor INY-06-086 and the original ERK5 inhibitor BAY-885.
    INY-06-061-induced ERK5 degradation is dependent on the ubiquitin-proteasome system.
    INY-06-061 treatment does not compromise viability in multiple cancer cell lines, does not affect pro-inflammatory cytokine secretion in endothelial cells.

    物理化学性质&存储条件

    分子量 1041.249
    分子式 C54H67F3N10O6S
    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

    (2S,4R)-1-((S)-2-(6-(4-(4-(1-(2-amino-4-(trifluoromethoxy)benzoyl)piperidin-4-yl)quinazolin-7-yl)piperazin-1-yl)hexanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

    参考文献

    1. Inchul You, et al. Cell Chem Biol. 2022 Oct 6;S2451-9456(22)00352-X.

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