k-80003

Product Namek-80003
CAS1292821-90-9
MFC22H21FO2
MW336.4
EINECS
MOL File1292821-90-9.mol

Chemical Properties

Boiling point	491.6±40.0 °C(Predicted)
Density	1.192±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 30 mg/mL (89.18 mM)
pka	4.27±0.10(Predicted)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

Uses

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

Definition

ChEBI: [5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid is a sulindac-based non-steroidal anti-inflammatory drug. It has a role as a non-steroidal anti-inflammatory drug. It is functionally related to an acetic acid.

in vivo

K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity^[1].

References

[1] Zhou H, et al. NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling. Cancer Cell. 2010 Jun 15;17(6):560-73. DOI:10.1016/j.ccr.2010.04.023
[2] Chen L, et al. Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα. Nat Commun. 2017 Jul 17;8:16066. DOI:10.1038/ncomms16066