Category: Leukemia

S2116 is a Potent Lysine-Specific Demethylase 1 (LSD1) Inhibitor

Lysine-specific demethylase 1 (LSD1) is a human protein encoded by the kdm1a gene. Specifically, LSD1 is a flavin-dependent monoamine oxidase that demethylates monomethyl and dimethyllysine, especially H3K4 and H3K9. Besides, LSD1 regulates a variety of biological processes through dual function regulation of enhancer function. Overexpression of LSD1 is a...

M-808 is a Highly Potent and Efficacious Covalent Menin-MLL Interaction Inhibitor

Menin is a putative tumor suppressor associated with multiple endocrine tumor type 1 (MEN-1 syndrome). Specifically, Menin has two functional nuclear localization signals and inhibits JunD transcriptional activation. MLL1, a histone methyltransferase, is an active global regulator of gene transcription. Besides, the protein belongs to histone-modifying enzyme and contains...

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...