ML 347

ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs. ALK3.IC50 value:Target: ALK1/ALK2ML347 has IC50’s of 46 and 32 nM, respectively, against ALK1 and ALK2; however, the IC50 against ALK3 is 10,800 nM, >300-fold selective over ALK3. ML347 is completely inactive against allthe other kinases tested (with weak activity against ALK6, 9830 nM and KDR (VEGFR2)19,700 nM). ML347 is potent in the BMP4 cell assay (152 nM).

Signaling Pathways >> TGF-beta/Smad >> TGF-β Receptor

Research Areas >> Cancer

[1]. Engers DW, et al. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.

SB431542 | Galunisertib (LY2157299) | A 83-01 | LY2109761 | LDN193189 | RepSox | SB525334 | Vactosertib (TEW-7197) | DMH-1 | GW788388 | LY364947 | SB505124 | LY3200882 | H-Leu-Ser-Lys-Leu-NH2 trifluoroacetate salt | ITD-1