ML-00253764 is a Brain Penetrant Melanocortin Receptor 4 Antagonist
The involuntary weight loss that occurs as some diseases poses a serious medical problem. For example, sarcopenia, cancer cachexia, rheumatoid arthritis, and hip fractures can lead to involuntary weight loss. The melanocortin 4 receptor (MC4R) plays a key role in body weight regulation and energy homeostasis. The signaling of...
AZD1208 is an Orally Bioavailable and Highly Selective PIM Kinases Inhibitor
Pim kinases, also known as serine/threonine kinases, have three highly homologous isoforms namely Pim-1, Pim-2, and Pim-3. And Pim-1, Pim-2, and Pim-3 are recurrent proviral integration locus in Moloney murine leukemia virus. The overexpression of Pim kinases occurs when viral inserts at this site. Pim kinases are overexpressed in...
SB-332235 is an Orally Active CXCR2 Antagonist
Chemokines are low m.w. proteins that modulate the immune response through the chemoattraction and activation of leukocytes. These mediators have four classes. Chemokines in which the first two cysteines are separated by a single, nonconserved amino acid are CXC or chemokines, while those containing adjacent N-terminalcysteine residues are CC ...
LYN-1604 is a Potent ULK1 Activator
UNC-51 like kinase 1 (ULK1) is the mammalian homolog of ATG1. ULK1 is an autophagic initiator that may decide the subsequent cell fate. In the autophagic process, ULK1 is a component of the ULK complex that is essential for autophagy induction in different types of cancer. Additionally, characterization of ULK1 expression...
MS049 is a Selective and Dual Inhibitor of PRMT4 and PRMT6
Protein arginine N-methyltransferase 4 (PRMT4) methylation of arginine residues in proteins plays a key role in transcriptional regulation. Specifically, PRMT4 binds to transcription activators called p160 and CBP/P300. Besides, the modified forms of these proteins are involved in the stimulation of gene expression through steroid hormone receptors. Moreover, PRMT4...
L-Moses Disrupts PCAF-Brd Histone H3.3 Interaction
Bromodomains proteins (Brds) bind to acetylated lysines (KAc) through the Brd acetyllysine-binding site. Misregulation of these proteins is linked to the onset and progression of multiple disease states. They include cancer, HIV infection, and neuroinflammation. The p300/CBP-associated factor, PCAF (KAT2B), is a multi-domain protein. It contains a single Brd,...
Miransertib is an Orally Active, Selective and Allosteric Akt Inhibitor
The AGC kinases AKT1, AKT2, and AKT3 are key mediators of the PI3K/AKT/mTOR signaling pathway. Additionally, AKT promotes diverse physiological processes, including cell proliferation, migration, and protein synthesis, et al. In this article, we will introduce an allosteric Akt inhibitor, Miransertib. As a potent inhibitor, Miransertib exhibits IC50s of...