Month: August 2020

UC2288 is an Orally Active p21 Attenuator

p21 is a member of the cip/kip family of cyclin-dependent kinase inhibitors, it regulates cell growth in both malignant or non-malignant cells. It possesses diverse physiological functions in vitro, such as vascular smooth muscle cell proliferation, cancer progression, and viral infection. p21 is well-known as a tumor suppressor protein...

CYH33 is an Orally Active and Highly Selective PI3Kα Inhibitor

PI3Ks are a class of enzymes involved in cell function, such as cell growth, proliferation, differentiation, movement, survival, and intracellular transport. And these cells are relevant to cancer. Specifically, I3K is a kind of related intracellular signal transduction enzymes, which can phosphorylate the 3-hydroxy group of phosphatidylinositol (PtdIns). In...

KCC-07 is a Selective and Brain-Penetrant MBD2 Inhibitor

Medulloblastoma (MB) is the most common and aggressive malignant brain tumor in children. MB has four clinically and molecularly distinct subgroups, and they are wingless (WNT) group, the sonic hedgehog (SHH) group, group 3, and group 4. In human MBs, TP53 mutations are frequent in the WNT and SHH...

MCP110 is an Inhibitor of Ras/Raf-1 Interaction

Ras is a small GTPase and interacts with the protein Raf to create activated Ras-Raf complex that activates the downstream effectors in the ERK pathway. Malfunctioning Ras-Raf switches cause cancer. Ras-Raf interaction has taken a center stage in cancer research. Ras is a peripheral membrane protein that acts as...

MS117 is a First-in-Class and Irreversible PRMT6 Covalent Inhibitor

PRMT6 is a protein arginine methyltransferase responsible for histone H3 arginine 2 (H3R2) methylation. PRMT6 negatively regulates DNA methylation and that PRMT6 upregulation contributes to global DNA hypomethylation in cancer. Mechanistically, PRMT6 overexpression impairs the chromatin association of UHRF1, resulting in passive DNA demethylation. Especially, PRMT6 plays an important...

DM-01 is a Powerful and Selective EZH2 Inhibitor

Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and a...

JX06 is a Potent, Selective and Covalent Inhibitor of PDK

Pyruvate dehydrogenase kinase (PDK) is a kinase that can be inactivated by the use of ATP phosphorylation of pyruvate dehydrogenase. Specifically, PDK is relevant to the regulation of the pyruvate dehydrogenase complex with pyruvate dehydrogenase as the first component. Besides, PDK acts as a molecular switch to reduce mitochondrial...