Category: Leukemia

DB1976 is a Fully Efficacious Transcription Factor PU.1 Inhibitor

ETS transcription factors mediate a wide array of cellular functions and are attractive targets for pharmacological control of gene regulation. Transcription factors (TFs) are central to many cellular processes and account for 5-10% of genes in eukaryotes. Besides, sequence-specific binding is an obligate step in ETS-mediated gene activation. So...

A-366 is a Potent Histone Methyltransferase G9a Inhibitor

Epigenetic alterations to the genome take place via modifications to the DNA or histones. Meanwhile, those modifications lead to changes in gene expression. Generally, histone lysine methylation is a prominent kind of epigenetic regulation for change of the structure chromatin and gene expression. HMTs have recently generated increasing interest...

CKI-7 is a Dual CK1 and Cdc7 Kinase Inhibitor

Protein phosphorylation plays a fundamental role in the regulation of a variety of cellular processes. Casein kinase I (CK1) is a cyclic nucleotide independent kinase. It is highly purified from various tissues, including calf thymus, rabbit reticulocytes, liver, and skeletal muscle. The widespread distribution of CK1 suggests its importance...

MG-277, a PROTAC Molecular Glue, Exhibits Anti-cancer Activity by Inhibiting GSPT1

Proteolysis targeting chimeras (PROTACs) induce protein degradation. A typical PROTAC small-molecule degrader consists of three essential components: a ligand that binds the protein of interest, a second ligand that binds to and recruits an E3 ligase degradation complex, and a linker tethering the two ligands together. MD-222, a bona...

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...

BY27 is a Selective and Orally Active BET BD2 Inhibitor

BET (Bromodomain and extra terminal domain) is a well-known member of the bromodomain family. It contains BRD2, BRD3, BRD4, and BRDT, which have two tandem bromodomains (BD1 and BD2). BD1 and BD2 are recognition motifs for the acetyl-lysine residues of N terminuses of histones as well as other proteins....

MD-224 is a First-in-Class and Highly Potent PROTAC Degrader of MDM2

As previously introduced, the tumor suppressor p53 plays a critical role in the prevention of tumor development. While human, murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53. And it has been pursued as a promising cancer therapeutic target. A study...