A retinoic acid analog and selective RARα agonist

AC261066 (AC-261066, AC261) is a potent, selective, orally available RARβ2 agonist with pEC50 of 8.1, displays selectivity over RARβ1, RARα and RARγ (pEC50=6.4, 6.2 and 6.3).

AR7 is a retinoic acid receptor α (RARα) antagonist.

CD437 is a synthetic retinoid that is an RARγ-selective agonist. It displays RARγ-dependent and -independent effects on differentiation and apoptosis.

Fenretinide (4-HPR) is a synthetic retinoid deriverative. 4-HBR is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

HX600 (HX-600) is a synthetic agonist of RXR-Nurr1 heterodimer complex, also selectively activate NGFI-B/RXR heterodimers.

LY2955303 is a potent and selective RAR-gamma antagonist for the treatment of osteoarthritis pain.

UAB30 (9cUAB30) is a novel synthetic rexinoid that binds selectively to the retinoid X receptor (RXR) leading to activation of genes involved in induction of differentiation and apoptosis.

Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with high affinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research.

CD3254 a potent and selective retinoid-X-receptor (RXR) agonist.

CD2665 is a selective RAR-beta/gamma antagonist, with Ki values of 110 nM, 306 nM for RARγ and RARβ, respectively.

PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.

LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.

Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.

Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

16α-Hydroxytrametenolic acid, a natural triterpene, is a potential retinoid X receptor (RXR) selective agonist.