Tag: MCF-7

MS4322 is a First-in-Class PRMT5 PROTAC Degrader

PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...

HS-131 is a near Infrared Dye Tethered Hsp90 Inhibitor

Hsp90 (heat shock protein 90) is a molecular chaperone protein. Specifically, Hsp90 can help other proteins fold correctly, stabilize proteins, resist heat stress, and contribute to protein degradation. It can also stabilize many proteins needed for tumor growth. Besides, Hsp90 is present in all branches of bacteria and eukaryotes....

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....

Elacestrant is an Orally Available SERD (Estrogen Receptor Degrader )

Estrogen receptor (ER) is a ligand-induced intracellular transcription factor that mediates the biological effects of estrogen at the level of most gene regulation. The biological effect of estrogen is mediated by ER, which is a member of nuclear receptor family. Specifically, these receptors act as ligand-activated transcription factors. There...

PF-06843195 is a Selective PI3Kα Inhibitor

Phosphoinositide 3-kinases (PI3Ks) can catalyze the synthesis of the phosphatidylinositol (PI) second messengers, including PI(3)P (PIP), PI(3,4)P2 (PIP2), and PI(3,4,5)P3 (PIP3). The PI3K lipid kinase family contains three classes based on sequence homology. Class, I PI3Ks are further divided into class IA (PI3Kα, PI3Kβ, and PI3Kδ) and class IB...