LDN193189 is a Selective BMP Type I Receptor Inhibitor

Fibrodysplasia ossificans progressiva (FOP) is a congenital disorder of progressive. It is widespread postnatal ossification of soft tissues and is without known effective treatments. A recent study identified heterozygous mutations in ACVR1, the gene encoding the BMP type I receptor ALK2, in all affected members from seven families. BMP...

Stafib-1 is the First Selective Inhibitor of the STAT5b SH2 Domain

The transcription factor STAT5A/B controls leukemic cell survival and disease progression. Especially, STAT5B as major STAT5 isoform driving BCR/ABL+ leukemia. Besides, STAT5B enables transformation by suppressing IFN-α/γ, thereby facilitating leukemogenesis. STAT5b might serve as an anticancer target in ductal pancreatic adenocarcinoma. Stafib-1 acts as the first selective inhibitor of...

PF-06260414 is an Orally Active and Nonsteroidal Selective Androgen Receptor Modulator

The Androgen receptor (AR) is a nuclear receptor. The Androgen receptor is a DNA binding transcription factor that regulates gene expression. Specifically, androgen-regulated genes are essential for the development and maintenance of male sexual phenotypes. Besides, androgen causes slow maturation of bone, but the more effective maturation comes from...

LC-2 is a First-in-Class PROTAC-Based KRAS G12C Degrader

KRAS gene is one of the most frequently mutated oncogenes in cancer. KRAS encodes a small, membrane-bound GTPase that relays signals from receptor tyrosine kinases (RTKs). It promotes cell proliferation, cell differentiation, or cell survival. In normal cells, KRAS functions as a molecular switch, cycling between an inactive, GDP-bound “off” state and...

DC_AC50 is a Dual inhibitor of Atox1 and CCS (Copper Chaperones)

Copper is a redox-active transition metal critical for most living organisms. At the same time, it serves as a catalytic cofactor for enzymes. Those enzymes play roles in antioxidant defense, iron homeostasis, cellular respiration, and a variety of biochemical processes. However, intracellular free copper may exhibit toxic side effects....

Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor

ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...

FLTX1, a Fluorescent Tamoxifen Derivative, Specifically Labels Intracellular Binding Sites (ER)

Tamoxifen is a nonsteroidal agent and competitively binds to estrogen receptors (ER). This compound itself is a prodrug and it has a relatively little affinity for ER. However, tamoxifen can transform into active metabolites 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen (endoxifen). Besides, these metabolites exhibit 30–100 times more affinity with the estrogen...