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首页-抗体药物偶连体和PROTACs-PROTAC-KH-103
KH-103

Chemical Structure : KH-103

CAS No.:

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KH-103 (KH103)

货号: PC-21533Not For Human Use, Lab Use Only.

KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PROTAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggering and crosstalk inhibition.

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

    生物&药学活性

    KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PROTAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggering and crosstalk inhibition.
    KH-103 (1 uM) led to efficient and rapid degradation of GR cells within less than an hour in HEK293 cells.
    KH-103 shows highly efficient degradation at 10 nM, reaching almost full depletion at 100 nM.
    KH-103 shows efficient reversible degradation in various in-vitro models across tissue origins and species.
    KH-103 induces nuclear translocation without triggering GR-mediated gene activation.
    KH-103 blocks dexamethasone (DEX) effects with increased efficiency compared to other inhibitors.
    KH-103 treatment alone has no nonspecific transcriptional effects.
    KH-103 effectively depletes GR in the pituitary in vivo and impacts corticosterone levels.

    物理化学性质&存储条件

    分子量 833.01
    分子式 C46H61FN4O9
    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

    (8S,9R,10S,11S,13S,14S,16R,17R)-N-(10-(2-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-2-oxoethoxy)decyl)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxamide

    参考文献

    1. Gazorpak M, et al. Nat Commun. 2023 Dec 9;14(1):8177.

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