A selective ALK2 inhibitor (IC50 = 1.3 nM) that less potently inhibits ALK1 and ALK3 (IC50 = 2.4 and 85.8 nM

LDN-212854 – 25 mg

Brand:
Cayman
CAS:
1432597-26-6
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair. LDN-212854 inhibits ALK2 (IC50 = 1.3 nM) in preference to other BMP type I receptors, ALK1 (IC50 = 2.4 nM) and ALK3 (IC50 = 85.8 nM) and with over 1,500-fold selectivity against the closely related activin and TGF-β type I receptors (i.e., ALK4 and ALK5).{28826} It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC50 value of 10 nM.{28826} LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRβ kinases with IC50 values less than 100 nM.{28826}  

 

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Description

A selective ALK2 inhibitor (IC50 = 1.3 nM) that less potently inhibits ALK1 and ALK3 (IC50 = 2.4 and 85.8 nM, respectively) and demonstrates over 1,500-fold selectivity against the closely related activin and TGF-β type I receptors (i.e., ALK4 and ALK5); inhibits BMP6-induced osteogenic differentiation with an IC50 value of 10 nM

Formal name: 5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline

Synonyms: 

Molecular weight: 406.5

CAS: 1432597-26-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling

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