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K 02288

Names

[ CAS No. ]:
1431985-92-0

[ Name ]:
K 02288

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

Biological Activity

[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.


[Related Small Molecules]

SB431542 | Galunisertib (LY2157299) | A 83-01 | Brigatinib | LY2109761 | lorlatinib | LDN193189 | Alectinib (CH5424802) | RepSox | Entrectinib | SB525334 | Vactosertib (TEW-7197) | DMH-1 | GW788388 | LY364947

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
522.2±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C20H20N2O4

[ Molecular Weight ]:
352.384

[ Flash Point ]:
269.6±30.1 °C

[ Exact Mass ]:
352.142303

[ PSA ]:
86.83000

[ LogP ]:
3.13

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.614

Safety Information

[ Symbol ]:

GHS05, GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H318

[ Precautionary Statements ]:
P280-P301 + P310 + P330-P305 + P351 + P338 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds