MedChemExpress - Model K02288 -1431985-92-0

K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.

K02288

MCE China：K02288

Brand：MedChemExpress (MCE)

Cat. No.HY-12278

CAS：1431985-92-0

Purity：99.73%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.

In Vitro：K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC50 of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 μM[1]. K02288 binds to ALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs[2].

In Vivo：K02288 (1 μM) induces dysfunctional angiogenesis in a chick embryo CAM model[2].

IC50 & Target：IC50：1.8 nM (ALK1), 1.1 nM (ALK2), 34.4 nM (ALK3), 6.3 nM (ALK6), 302 nM (ALK4), 321 nM (ALK5)[1] Cellular Effect Cell Line Type Value Description References

References：

[1]. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721. [Content Brief]

[2]. Kerr G, et al. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17. [Content Brief]

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MedChemExpress - Model K02288 -1431985-92-0

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K02288