K 02288

Modify Date: 2024-01-02 10:54:16

K 02288 Structure
K 02288 structure
Common Name K 02288
CAS Number 1431985-92-0 Molecular Weight 352.384
Density 1.2±0.1 g/cm3 Boiling Point 522.2±50.0 °C at 760 mmHg
Molecular Formula C20H20N2O4 Melting Point N/A
MSDS Chinese USA Flash Point 269.6±30.1 °C
Symbol GHS05 GHS06
GHS05, GHS06
Signal Word Danger

 Use of K 02288


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.

 Names

Name 3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol
Synonym More Synonyms

 K 02288 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
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.

 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
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

 Synonyms

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