alk1

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.

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.

LDN-214117 is a potent and selective ALK2 inhibitor.

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.

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.

Ascrinvacumab (PF-03446962) is a highly humanized IgG2 monoclonal antibody against ALK-1 with a Kd value of 7 nM for human ALK1. It has an inhibitory effect on TGF-β and can be used to study hepatocellular carcinoma (HCC).

Compound 4, known as GALK1-IN-1, is a potent inhibitor of galactokinase, exhibiting an IC50 value of 4.2129 μM [1].

A2793 is a dual inhibitor of TWIK-associated acid-sensitive K+ channel 1 (TASK-1)/TRESK, with an IC50 for mTRESK of 6.8 μM. It is more selective for TRESK, and relatively weaker for TREK-1 and TALK-1.

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

LDN-193189 HCl (LDN193189 Hydrochloride) is a selective BMP type I receptor kinases inhibitor.

MU1700, an orally active and potent inhibitor targeting ALK1/2, exhibits IC50 values of 13 nM for ALK1 and 6 nM for ALK2. It demonstrates both cell membrane and high brain permeability.

M4K2234 (Compound 26b) is a selective inhibitor of ALK2, displaying IC50 values of 5 nM for ALK2 and 2144 nM for ALK5. As a chemical probe for ALK1 and ALK2 kinases, it is used in mechanistic studies of BMP signaling and in cancer research where dysregulated ALK2 activity is implicated. Its high selectivity profile supports targeted investigations into ALK-mediated pathways.

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).

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

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

CDD-2789 is a highly selective small molecule inhibitor that targets Activin receptor type 1 (ALK2, also known as ACVR1). It effectively blocks the BMP and activin A-induced downstream phosphorylation reactions by inhibiting the ALK2/ALK1-mediated SMAD1/5 signaling pathway. In the NanoBRET cell model, CDD-2789 demonstrates an inhibitory activity with an IC50 value of 0.54 µM for ALK2. This compound holds potential for research in ALK2-related diseases, including brainstem glioma (DIPG), ependymoma, endometrial cancer, melanoma, non-small cell lung cancer, colorectal cancer, and pancreatic cancer.

P7170 is an anti-cancer agent active as an mTORC1/C2 and activin receptor-like kinase 1 (ALK1) inhibitor.