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…
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…
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…
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…
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…
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…
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…
Senaparib is a Selective and Orally Active PARP1/2 Inhibitor
Poly(ADP-ribose) polymerase (PARP) is an important protein in DNA repair pathways especially the base excision repair. . PARP proteins compose of two ribose moieties and two phosphates per unit polymer.…
Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor
Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option…
NSC-105808 is a Specific DNA2 Nuclease Inhibitor with Antitumor Activity
DNA2 nuclease possesses 5′ flap endonuclease and 3′-5′ helicase activities. It has an important role in DNA damage repair, homologous recombination, and DNA replication. The nuclease activity of DNA2 has…