dCBP-1 is a Selective PROTAC Degrader of p300/CBP
The paralogous chromatin regulators CREB-binding protein (CBP) and p300 are factors critical for establishing and activating enhancer-mediated transcription. The CREB-binding protein (CBP) and p300 are important factors for activating enhancer-mediated transcription. These proteins consist of at least 10 distinct functional domains. Most of them interact with over 400 other proteins,...
MYCMI-6 is a Selective Endogenous MYC:MAX Inhibitor
The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables the MYC:MAX complex to bind E-box regulatory DNA elements throughout the genome. Therefore, it controls the transcription of a...
BI-9321, a First-in-Class Chemical Probe, is a NSD3-PWWP1 Inhibitor
Post-translational modification of histones by histone-modifying enzymes represents a key element of epigenetic regulation. Epigenetic reader domains are structurally diverse. They include bromodomains, PHD domains, methyl-lysine- and/or methyl-arginine-binding domains, frequently co-locating within the same proteins. By interfering with the function of specific domains, selective chemical probes represent powerful tools...
CMLD010509 is a Highly Specific Inhibitor of the Oncogenic MYC-Driven Translation Program
Multiple myelomas (MM) is a hematological malignancy, it exhibits a clonal proliferation of plasma cells in the bone marrow micro-environment. MM remains a frequently incurable hematological malignancy until today. MYC can directly enhance transcription genes encoding ribosomal proteins, ribosomal RNA, and proteins of the translation initiation complex. Furthermore, most...
sAJM-589 is a Myc Inhibitor by Disrupts the Myc-Max Heterodimer
The proto-oncogene Myc belongs to the basic helix-loop-helix leucine zipper (B-HLH-LZ) transcription factor family. It plays a key role in cellular proliferation, differentiation, and apoptosis. Myc expression is normally under tight control. Its expression is transient and responsive to mitogen stimulation. Indeed, in more than 70% of human malignancies,...
BI8622 is a HUWE1 Ubiquitin Ligase Inhibitor for Colorectal Cancer
HUWE1 is a colonic tumor suppressor. Especially, HUWE1 is a critical colonic tumour suppressor gene that prevents MYC signalling, DNA damage accumulation and tumor initiation.HUWE1 is a pleiotropic E3 ubiquitin ligase that modulates the function of several proteins involved in oncogenesis and DNA damage response including MYC, MYCN, MCL1...