LG100268

LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].

Product Specifications

CAS Number

[153559-76-3]

Product Name Alternative

LG268

UNSPSC

12352005

Target

Autophagy; RAR/RXR

Type

Reference compound

Related Pathways

Autophagy; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/lg-100268.html

Concentration

10mM

Purity

99.39

Solubility

DMSO : 5.56 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C2(C3=C(C)C=C4C(C)(C)CCC(C)(C)C4=C3)CC2)N=C1)O

Molecular Formula

C24H29NO2

Molecular Weight

363.49

References & Citations

[1]M F Boehm, et al. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem|[2]D S Lala, et al. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383 (6599) :450-3.|[3]Martine Cao, et al.The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila) . 2016 Jan;9 (1) :105-14.