BMS453 is a RARβ Agonist and a RARα/RARγ Antagonist
Retinoids inhibit the growth of many human tumor cells. Retinoids are ligands of retinoic acid receptors alpha, beta, gamma (RARs, α, β and γ). Retinoic acid receptors (RARs) are ligand-controlled transcription factors that function as heterodimers with retinoid X receptors (RXRs) to regulate cell growth and survival. BMS453 is...
BI99179 is a Selective Type I FASN Inhibitor
Fatty acid synthase (FASN) is a key enzyme involved in neoplastic lipogenesis. In particular, the Overexpression of FASN is common in many cancers. FASN is a metabolic oncogene with an important role in tumor growth and survival, making it an attractive target for cancer therapy. Especially, BI 99179 acts...
NVS-CECR2-1 is a CECR2 BRD (non-BET Family) Inhibitor
A Bromodomain (BRD) is a protein domain of about 110 amino acids and is a “reader” of lysine acetylation. Specifically, BRDs recognize acetylated lysine residues, such as those on the N-terminal tail of histones. Besides, BRD is responsible for the transduction of signals carried by acetylated lysine residues and...
ICCB280 is a Potent C/EBPα Inducer with Anti-Leukemic Properties
Knowledge of the pathogenesis of AML has seen great progress due to recent advances in genetic studies. However, the long-term survival of AML patients is still unsatisfactory. A block in differentiation is one of the characteristics of leukemia. C/EBPα is an essential transcription factor for the differentiation of cells...
JH-XI-10-02 is a Highly Potent and Selective PROTAC CDK8 Degrader
PROteolysis Targeting Chimeras (PROTACs) regulate protein function by degrading target proteins instead of inhibiting them, providing more sensitivity to drug-resistant targets. PROTACs show better selectivity compared to classic inhibitors. PRTOACs have outperformed not only in cancer diseases but also in immune disorders, viral infections, and neurodegenerative diseases. PROTACs present...
NU6102 is a Potent CDK1 and CDK2 Inhibitor
CDKs remain attractive targets for anti-proliferative cancer chemotherapy. they play a central role in cell division and growth. Amongst the cell cycle CDKs, CDK2 has attracted the most attention and its exploitation as a drug target based on structure-based drug design. In this article, we will introduce a potent...
CMLD-2 is Inhibits HuR and Induces Apoptosis
Hu antigen R (HuR) is an RNA binding protein. Specifically, Its overexpression in human cancer is associated with aggressive disease, drug resistance, and poor prognosis. HuR is highly abundant in many types of cancer and promotes tumorigenesis through cancer-related mRNA interactions. Besides, HuR has related to the regulation of...