alk2

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) (IC50: 9 nM), inhibiting ALK2 700-fold more than ALK3.

ALK2-IN-4 succinate is a robust and effective inhibitor of ALK2.

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.

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

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

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, demonstrating IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [1].

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

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

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 (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.

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.

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 BMP inhibitor.

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.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that effectively 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. Furthermore, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S and G1 phases in MCF7 and HCT116 cells, respectively, and triggers apoptosis effectively [1].

Prafnosbart (DS-6016A) is a humanized IgG1-kappa monoclonal antibody targeting ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1), utilized in research on bone metabolism disorders [1].

LDN193189 Tetrahydrochloride is a selective inhibitor of BMPI-type receptors and inhibits ALK2 (IC50: 5 nM) and ALK3 (IC50: 30 nM), with weak effects on ALK4, ALK5 and ALK7 (IC50 ≥ 500 nM).

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), an ALK2 inhibitor, demonstrates selective inhibition of ALK2 and ALK5 with IC50 values of 5 nM and 2144 nM, respectively. Serving as a chemical probe for ALK1 and ALK2 protein kinases, M4K2234 holds potential for cancer research applications [1].

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.

Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM).

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

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.

Itacnosertib hydrochloride acts as an inhibitor targeting JAK2, ACVR1 (ALK2), and ALK5 [1].

M4K2163 dihydrochloride, a potent and selective activin receptor-like kinase-2 (ALK2) inhibitor that is permeable to the blood-brain barrier (BBB), has an IC50 of 19 nM. This compound is useful in diffuse intrinsic pontine glioma (DIPG) research [1] [2].

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.

Itacnosertib (TP-0184) is a chemical compound that acts as an inhibitor of JAK2, ACVR1 (ALK2), and ALK5, as indicated in WO2014151871.

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.

RIPK2-IN-1 (compound 18f) is a potent inhibitor of RIPK2 (IC50: 51 nM) and also inhibits ALK2 (IC50: 5 nM).