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首页-抗体药物偶连体和PROTACs-PROTAC-WD6305
WD6305

Chemical Structure : WD6305

CAS No.:

WD6305 (WD 6305, WD-6305)

货号: PC-21676Not For Human Use, Lab Use Only.

WD6305 is a potent and selective proteolysis-targeting chimera (PROTAC) degrader of METTL3-METTL14 complex with DC50 of 140 nM (METTL3), Dmax of 91.9% in Mono-Mac-6 AML cell line.

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

    生物&药学活性

    WD6305 is a potent and selective proteolysis-targeting chimera (PROTAC) degrader of METTL3-METTL14 complex with DC50 of 140 nM (METTL3), Dmax of 91.9% in Mono-Mac-6 AML cell line.
    WD6305 caused a 71.4% degradation of METTL3 protein at 1 μM after 24h in Mono-Mac-6 cells, a METTL3-expressed AML cell line.
    WD6305 induced rapid degradation of METTL3 protein within 2 h and nearly completely abolished METTL3 protein after a 12-h treatment at 500 nM.
    WD6305 effectively reduced METTL14 protein level in a dose-dependent manner with a DC50 of 194 nM, with no significant effect on WTAP protein levels.
    WD6305 induces degradation of the METTL3-METTL14 complex through the ubiquitin-proteasomal system.
    WD6305 inhibits m6A modification and proliferation, and induces apoptosis in AML cell lines, has more potent anti-leukemic activity compared to its parent METTL3 inhibitor (UZH2, Cat#PC-49679).

    物理化学性质&存储条件

    分子量 1112.40
    分子式 C61H75F2N11O5S
    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-(5-(4-(((6-(4-(4-((4,4-dimethylpiperidin-1-yl)methyl)-2,5-difluorophenyl)-2-oxo-1,4,9-triazaspiro[5.5]undecan-9-yl)pyrimidin-4-yl)amino)methyl)phenyl)pent-4-ynamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

    参考文献

    1. Wenhao Du, et al. Cell Chem Biol. 2024 Jan 2:S2451-9456(23)00439-7.

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