alk2

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

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-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.

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

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.

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.

M4K2306 is a selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 7 nM. It is capable of penetrating the blood-brain barrier, exhibiting a brain-to-plasma ratio of 75.6.

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.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [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.