Category: Leukemia

TNP-351, an Antifolate, is a Dihydrofolate Reductase (DHFR) Inhibitor

Antifolates are a class of antimetabolite medications that block the actions of folic acid. Antimalarial antifolates have been central for prophylaxis and treatment of malaria. The success of antifolates in the treatment of tumors also leads to the use of this class of drugs in the treatment of other...

THZ-P1-2 is a Selective PI5P4K Inhibitor

Phosphatidylinositol 5-phosphate (PI-5-P) is one of the seven phosphoinositides. They regulate a wide range of cellular functions. They localize in the nucleus, Golgi, endoplasmic reticulum, and at the plasma membrane. PI-5-P is an oxidative stress-induced regulator of AKT activation. The phosphorylation of the low abundance phosphoinositide PI-5-P at the...

SNDX-5613 is a Potent and Specific Menin-MLL Inhibitor

Mixed lineage leukemia (MLL) is a very aggressive blood cancer that predominantly occurs in pediatric patients. Especially, MLL is acute leukemia with poor prognosis. Spontaneous translocations at the MLL1 gene cause MLL. MLL fusions bind with a high affinity to the nuclear protein Menin. Menin-MLL interaction enables leukemic transformation...

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...