Pelcitoclax (APG-1252) is a Bcl-2/Bcl-xl Inhibitor with Antineoplastic and Pro-Apoptotic Effects
Bcl-2 (B-cell lymphoma 2) is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). Particularly, the Bcl-2 and Bcl-xl...
GL0388 Activates Bax and Induce Bax-Mediated Apoptosis
Bax is a member of the bcl-2 gene family. Specifically, BCL2 family members are relevant to a variety of anti-apoptotic or pro-apoptotic regulators. The expression of this gene is regulated by the tumor suppressor gene p53. Besides, Bax interacts with mitochondrial voltage-dependent anion channel VDAC and induces its opening....
CCI-007 Possesses Anti-Cancer Activity against Infant MLL-Rearranged Leukemia
Leukemia, characterized by rearrangement of the mixed lineage leukemia (MLL) gene, is a highly aggressive cancer. And the infant leukemia is particularly common. However, the cure rate of infant leukemia has been stagnant in recent years. The occurrence of MLL gene rearrangement is a prognostic factor for high-risk diseases....
NU9056 is a Selective Tip60 (KAT5) Histone Acetyltransferase Inhibitor
Histone acetylation and deacetylation are key events in the regulation of chromatin structure. Additionally, Histone acetyltransferases (HATs) can catalyze acetyl groups to the ε-amino terminus of lysine residues within histones. Acetylation results in an open chromatin structure by removing positive charges from histones. As a result, it induces protein...
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...
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...
Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor
Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...