PR-104A is a Hypoxia-Selective DNA Cross-Linking Agent and Cytotoxin
PR-104, like TH-302, is a prodrug of nitrogen mustard that has shown some degree of efficacy in adult patients with relapsed/refractory acute myeloid leukemia (AML). PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Therefore, this compound...
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...
EB-3D, a ChoKα1 Inhibitor, Induces AMPK-mTOR Pathway Deregulation and Apoptosis
T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematologic disorder. It results from the malignant transformation of T-cell progenitors. Since the overexpression of choline kinase alpha 1 (ChoKa1) has been associated with tumorigenesis in many cancers, it becomes an interesting therapeutic target. ChoK catalyzes the phosphorylation of choline (Cho)...