alk 2

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-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].

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.

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

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.

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

ALK/ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

PROTACALK degrader-2 (B1-PEG) is a PROTAC-based ALK degrader with a DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). Through PEGylation, PROTACALK degrader-2 can self-assemble into micelles in water, releasing its active form in tumor-specific high-GSH environments.

ALK degrader 2 is an orally active ALK degrader that reduces EML4-ALK protein levels (DC50= 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50= 102 nM). It facilitates ALK degradation through the Hsp70 chaperone system and the ubiquitin-proteasome pathway. In H3122 cells, ALK degrader 2 causes significant cell cycle arrest at the S phase and induces apoptosis. Additionally, it demonstrates antitumor activity in mice with H3122 xenograft tumors. ALK degrader 2 is a useful compound in researching non-small cell lung cancer (NSCLC).

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

ALK/EGFR-IN-2 is a potent dual inhibitor targeting ALK and EGFR, promoting apoptosis and G0/G1 cell cycle arrest in cancer cells. It effectively suppresses proliferation in H1975, PC9, and Baf3-EML4-ALK cancer cell lines, with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [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.