Histone Demethylase Degrader
-
LD-110 triTFA
0 ImagesCat. No.: HY-178825APurity: 99.77%LD-110 triTFA is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 triTFA acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 triTFA induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 triTFA inhibits tumor growth in the KYSE-150 xenograft model. LD-110 triTFA can be used in research related to esophageal squamous cell carcinoma.
-
LD-110 trihydrochloride
0 ImagesCat. No.: HY-178825BLD-110 trihydrochloride is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 trihydrochloride acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 trihydrochloride induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 trihydrochloride inhibits tumor growth in the KYSE-150 xenograft model. LD-110 trihydrochloride can be used in research related to esophageal squamous cell carcinoma.
-
PROTAC KDM3 degrader-1
0 ImagesPROTAC KDM3 degrader-1 is a KDM3A/KDM3B PROTAC degrader with DC50 values of 13.73 nM and 172.6 nM in SW480 cells, respectively. PROTAC KDM3 degrader-1 induces cereblon-dependent proteasomal degradation of KDM3A and KDM3B. PROTAC KDM3 degrader-1 inhibits the oncogenic Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 eliminates colorectal cancer stem cells, suppresses their self-renewal, and blocks colony formation of colorectal cancer cells. PROTAC KDM3 degrader-1 inhibits tumor growth in a colorectal cancer xenograft mouse model. PROTAC KDM3 degrader-1 can be used for the research of colorectal cancer.
-
GT-653
0 ImagesGT-653 is a selective KDM5B PROTAC degrader. GT-653 induces ubiquitination and degradation of KDM5B without altering the transcriptional level of KDM5B. GT-653 upregulates the level of H3K4me3. GT-653 activates the type I Interferon signaling pathway. GT-653 can be used for the research of prostate cancer.
-
LD-110
0 ImagesCat. No.: HY-178825LD-110 is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 inhibits tumor growth in the KYSE-150 xenograft model. LD-110 can be used in research related to esophageal squamous cell carcinoma.
-
PROTAC KDM4 degrader-1
0 ImagesPROTAC 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.
-
DW-229
0 ImagesCat. No.: HY-183618DW-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.
