diffuse intrinsic pontine glioma(dipg)

LDN-214117 is a potent and selective ALK2 inhibitor.

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].

Compound BPP (HDGFRP2 PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

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).

MTX-241F, a selective small molecule inhibitor, targets members of the EGFR and PI3 kinase families. It penetrates the blood-brain barrier, providing long-term tumor growth control and exhibits radiosensitizing activity in patient-derived DIPG neurospheres, potentially beneficial for studying diffuse intrinsic pontine glioma (DIPG) [1].