blm-in-1

BLM-IN-1 is a potent inhibitor of Bloom syndrome protein (BLM) with a KD of 1.81 μM and IC50 of 0.95 μM. It induces DNA damage response, apoptosis, and proliferation arrest in cancer cells.

Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.

ATUX-1215, a protein phosphatase 2A (PP2A) activator, diminishes the phosphorylation of ERK, p38, JNK, and Akt, as well as decreases the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals, potentially decelerating lung fibrosis progression [1].