Drug intelligence / Profile preview

LDN193189

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal (preclinical Animal Studies)
01

Overview

LDN193189 is a potent and selective small molecule inhibitor of the bone morphogenetic protein (BMP) pathway. It acts primarily by inhibiting BMP type I receptors ALK2 (ACVR1), ALK3 (BMPR1A), as well as ALK1 and ALK6 to a lesser extent. The compound prevents phosphorylation of Smad1/5/8 proteins downstream of BMP signaling. It was derived from structure–activity relationship studies of dorsomorphin and exhibits high selectivity for BMP signaling over TGF-beta signaling (>200-fold). LDN193189 is widely used in research to modulate stem cell differentiation—especially neural induction—and has been studied in animal models for conditions such as fibrodysplasia ossificans progressiva (FOP), ectopic ossification, and cancer. It is not approved for human or veterinary therapeutic use; it is intended strictly for research applications[1][3][4][8].

Brand names
Stemolecule LDN-193189
Other names
4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline hydrochloride4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline hydrochloride
02

Targets

ACVR1 (Activin receptor type I)TGFBR1ACVR1C (Activin A Receptor Type 1C)ACVR1B (Activin A receptor type IB)BMPR1A

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