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首页-抗体药物偶连体和PROTACs-PROTAC-YX968
YX968

Chemical Structure : YX968

CAS No.: 2742732-92-7

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YX968 (YX-968, YX 968)

货号: PC-21143Not For Human Use, Lab Use Only.

YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).

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

    生物&药学活性

    YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).
    YX968 induces highly potent, rapid, and selective degradation of both HDAC3/8 without triggering pan-HDAC inhibitory effects.
    YX968 shows HDAC1 and HDAC3 enzyme inhibition (IC50 = 591 nM and 284 nM, respectively).
    YX968 rapidly degrades HDAC3 and HDAC8 via the ubiquitin-proteasome system (UPS).
    YX968 is highly specific in targeted HDAC3/8 degradation, with no effect on HDAC2, HDAC4, HDAC6, and HDAC7.
    YX968 does not significantly alter transcriptome.
    YX968 is highly potent on suppressing the growth of cancer cell lines, YX968 (125 nM) estrogen receptor-positive BC cell lines MCF7 and T47D as well as the TNBC cell lines BT549, MDA-MB-468 and HCC1806.

    物理化学性质&存储条件

    分子量 831.13
    分子式 C45H66N8O5S
    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)-3,3-dimethyl-2-(8-(4-(4-(2-propylhydrazine-1-carbonyl)phenyl)piperazin-1-yl)octanamido)butanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

    参考文献

    1. Yufeng Xiao, et al. Cell Chem Biol. 2023 Aug 8;S2451-9456(23)00240-4.

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