We are happy to continue our series of posts which are inspired by Drug Hunter’s “Molecules of the Month”!
Here are two molecules that were recently highlighted by Drug Hunter!

1. Inavolisib (GDC-0077) is an oral, potent, and selective inhibitor of mutant α-isoform of phosphoinositide 3-kinase (PI3Kα). Dysregulations in the PI3K pathway are frequently present in HR+ breast cancer. They are usually caused by mutations in genes that code pathway enzymes, including PI3K. Inavolisib binds to the ATP-binding site of PI3Kα, which leads to inhibiting phosphorylation of PIP2 to PIP3 and prevents signaling in PI3K pathway. Besides inhibiting, inavolisib acts as a selective degrader of the mutant p110α protein, the catalytic subunit of PI3Kα. This drug candidate with benzoxazepin-oxazolidinone moiety is in a Ph. III for treating patients with PIK3CA-mutant breast cancer.

You can find the analogs to this molecule here!

2. DN-1289 is an orally available, selective, and blood-brain barrier penetrating dual inhibitor of leucine zipper kinase (DLK) and leucine zipper-bearing kinase (LZK). Both these kinases, DLK and LZK, are regulators of neuronal degeneration and axon growth and are known as targets of interest for neurodegenerative diseases, e.g., Alzheimer's disease (AD), Parkinson’s disease (PD), and Amyotrophic lateral sclerosis (ALS). DN-1289 demonstrates excellent in vivo plasma half-life and freely penetrates the CNS with no brain damage. Based on in vivo rodent studies and human in vitro models, DN-1289 shows promising neuroprotective properties in models of ALS.

You can find the analogs to this molecule here!

Use chem-space.com/search to find off-the-shelf and Make-on-Demand molecules of your interest!