1. Signaling Pathways
  2. Epigenetics
  3. Histone Demethylase
  4. Histone Demethylase Degrader

Histone Demethylase Degrader

Histone Demethylase Degraders (8):

Cat. No. Product Name Effect Purity
  • HY-178825A
    LD-110 triTFA
    Degrader 99.56%
    LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer.
  • HY-178825B
    LD-110 trihydrochloride
    Degrader
    LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer.
  • HY-168593
    PROTAC KDM3 degrader-1
    Degrader 99.07%
    PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547).
  • HY-158432
    GT-653
    Degrader 99.84%
    GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
  • HY-178825
    LD-110
    Degrader
    LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer.
  • HY-173135
    PROTAC KDM4 degrader-1
    Degrader
    PROTAC KDM4 degrader-1 is a KDM4 PROTAC degrader that degrades KDM4A-C with DC50 values of 37.53, 39.93, and 49.41 nM, respectively, while sparing KDM4D. PROTAC KDM4 degrader-1 induces cell cycle arrest, apoptosis and antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 can be used for the research of esophageal cancer.
  • HY-183618
    DW-229
    Degrader
    DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer.
  • HY-175036
    YTHu78
    Degrader
    YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).