alk2

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, demonstrating 700-fold higher inhibition of ALK2 compared to ALK3.

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.

KER047 (ALK2-IN-4) is an ALK2 inhibitor with potential anticancer activity and can be used in the study of non-small cell lung cancer.

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.

OD36 is a selective and potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 inhibits ALK2 signaling and osteogenic differentiation (KD: 37 nM), and binds efficiently to the ALK2 kinase ATP pocket.

OD36 hydrochloride (OD-36 hydrochloride) is a potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 hydrochloride is a macrocyclic inhibitor that binds efficiently to the ATP pocket of the ALK2 kinase and effectively antagonizes mutant ALK2 signaling and osteogenic differentiation.OD36 hydrochloride targets ALK2. OD36 hydrochloride targets ALK2 with a KD of 37 nM.

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.

Zilurgisertib (INCB-000928) is a selective and potent ALK 2 inhibitor for the study of cancer and MF anemia.

Blu-782 (ALK2-IN-1) is a activin receptor-like kinase-2 (ALK2) inhibitor ( IC50 of <10 nM)

ALK2-IN-4 succinate is a potent and effective inhibitor of ALK2 (ActRI), providing significant promise for therapeutic uses [ActR-1].

ALK2-IN-5, a pyrazolopyrimidine compound, serves as an inhibitor of ALK2 and FGFR, targeting disorders linked with their activity, including cancer [1].

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.

LDN 193688 is a BMP kinase inhibitor preferential for the ALK2 site, acting by binding to the ALK site, with BMP inhibitory activity 100 times that of TGFβRI, used in the study of progressive osseous fibrodysplasia.

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

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability.

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

M4K2308, a selective ALK2 ether-linked inhibitor, demonstrates an IC50 of 2 nM and exhibits greater specificity for ALK2 over ALK5, with an IC50 of 224 nM for ALK5. This compound holds potential for research into Diffuse Intrinsic Pontine Glioma (DIPG).

M4K2281 is a potent and selective inhibitor of ALK2 with a half-maximal inhibitory concentration (IC50) of 2 nanomolar. In both biochemical and cellular assays, M4K2281 and M4K2308 demonstrate strong efficacy against ALK2. Moreover, M4K2281 exhibits a brain-to-plasma ratio that ranges from moderate to high.

M4K2009 is a selective and brain-penetrant ALK2 inhibitor (IC50 = 13 nM) effective against both wild-type (WT) and mutant ALK2 (G328V, R206H, and R258G), used for the treatment of diffuse intrinsic pontine glioma (DIPG).

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.