1431985-92-0

1431985-92-0 structure

Name: K 02288
Chemical Name: 3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol
CAS Number: 1431985-92-0
Molecular Formula: C₂₀H₂₀N₂O₄
Molecular Weight: 352.384
Catalog: Biochemical Inhibitor TGF-beta/Smad signaling pathway inhibitor (TGF-beta/Smad) TGF-beta/Smad inhibitor
Create Date: 2018-12-24 15:11:40
Modify Date: 2024-01-02 10:54:16
K02288 is a potent inhibitor of ALK, and inhibits ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; K02288 is less potent against ALK4/5, with IC50s of 302 nM and 321 nM.

Name	3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol
Synonyms	3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol Phenol, 3-[6-amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]- K02288

Description	K02288 is a potent inhibitor of ALK, and inhibits ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; K02288 is less potent against ALK4/5, with IC50s of 302 nM and 321 nM.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK Signaling Pathways >> TGF-beta/Smad >> TGF-β Receptor Research Areas >> Others
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]
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].
References	[1]. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721. [2]. Kerr G, et al. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17.