DCH36_06 is a Selective p300/CBP Inhibitor
Histone acetyltransferases (HATs) are epigenetic enzymes that relieve transcriptional repression by preferentially acetylation of ε-amino group of lysine residues on histones. In general, HATs are crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells. HATs can be grouped into at least five different subfamilies (HAT1, Gcn5/PCAF, MYST, p300/CBP,...
SJ6986 is a Selective and Orally Active GSPT1/2 Degrader
Targeted protein degradation (TPD) is a novel chemical biology approach. Molecular glues (MGs) are small molecules that can bind to E3 ligase and change their surface and specificity, leading to the recruitment, ubiquitination, and subsequent degradation of substrates that are normally not targeted by the ligase (neosubstrates). Immunomodulatory imide...
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....
Rosabulin is a Potent Microtubule Inhibitor
Chemotherapy is a cornerstone in the development of present-day cancer therapy. Moreover, Chemotherapy is one of the most effective and potent strategies to treat malignant tumors. However, Chemotherapy resistance occurs when cancers that have been responding to therapy suddenly begin to grow. Rosabulin is a potent tubulin inhibitor. In...
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...
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...
Piclidenoson is a First-in-Class and Orally Active A3AR Agonist
One of the main strategies for cancer research is the identification of drugs that can cause apoptotic death in malignant cells. Additionally, Adenosine 5′-triphosphate (ATP), UTP, and adenosine are considered that inhibit the growth of several cancerous cell lines. Adenosine has several physiological and pharmacological functions. It can modulate...