Epigenetic Reader Domain Degrader

iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models.

RB-CO-PEG5-C2-CO-VH032 is a VHL-recruiting TRIM24 PROTAC degrader composed of an RB-derived short peptide SPRT, a PEG5-C2 linker, and the VHL ligand VH032. RB-CO-PEG5-C2-CO-VH032 recognizes proteins containing the FXXXV motif and recruits VHL to induce degradation of proteins such as TRIM24, thereby upregulating DUSP2, inhibiting ERK/mTOR signaling, and suppressing prostate cancer cell proliferation. RB-CO-PEG5-C2-CO-VH032 can be used for TRIM24 degradation and prostate cancer-related research.

PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL).

MS479 is a PROTAC degrader targeting BRD4, BRD3 and BRD2. MS479 recruits the E3 ligase SPOP by bridging the protein GLP, thereby promoting polyubiquitination modification and subsequent 26S proteasomal degradation. MS479 inhibits the proliferation of colorectal cancer cells and can be used for research on colorectal cancer and triple-negative breast cancer.

LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.

SYC-2863 is a CRBN-recruiting PROTAC degrader that selectively degrades ENL (MLLT1), with an ENL DC₅₀ of 45 nM in MV4;11 cells. SYC-2863 inhibits the proliferation of MLL-rearranged leukemia and multiple myeloma cells. After degrading intracellular ENL, SYC-2863 dose-dependently downregulates the transcription levels of MYC and its downstream target genes, blocking the MYC-mediated malignant proliferation pathway. SYC-2863 can be used in studies related to MLL-rearranged leukemia and multiple myeloma.

PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).

JP-2-196 is a molecular glue that covalently targets the RING family E3 ligase RNF126. JP-2-196 also binds to RNF40, MID2, RNF219, RNF14, and LRSAM1. JP-2-196 induces the formation of ternary complexes between RNF126 and target proteins (e.g., BRD4, AR-V7), thereby promoting their ubiquitination and proteasomal degradation. JP-2-196 has potential for cancer research (such as prostate cancer and leukemia).

dBET6 (Standard) is the analytical standard of dBET6 (HY-112588). This product is intended for research and analytical applications. dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 14 nM, and has antitumor activity.