transforming growth factor beta receptors

SB-431542 is an inhibitor of ALK5 TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

RepSox (ALK5 Inhibitor II) is a TGFβR-1 ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23 4 nM). RepSox induces adipogenesis in MEFs cells.

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1 3 compared to other inhibitors.

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

ML347 (LDN 193719)(DN193719) is a highly specific ALK1 2 inhibitor ( IC50: 46 32 nM), and the selectivity for ALK2 is >300-fold than ALK3.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.

BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)

SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.

LY2109761 is a novel selective TGF-β receptor type I II (TβRI II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.

SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.

Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

Maohuoside A promotes osteogenesis of rat mesenchymal stem cells via BMP and MAPK signaling pathways.

GW788388 is a potent and selective inhibitor of ALK5, and it also inhibits TGF-(beta) type II receptor and activin type II receptor activities.

K 02288 is a novel small molecule inhibitor of ALK1 2 3 6.