LE135

LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively[1][2].

Product Specifications

CAS Number

[155877-83-1]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

RAR/RXR; TRP Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/le135.html

Concentration

10mM

Purity

99.0

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(O)C1=CC=C(C2=NC3=CC4=C(C(C)(C)CCC4(C)C)C=C3N(C)C5=CC=CC=C52)C=C1

Molecular Formula

C29H30N2O2

Molecular Weight

438.56

Precautions

H315, H319

References & Citations

[1]H Umemiya, et al. Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem. 1997 Dec 19;40 (26) :4222-34.|[2]Shijin Yin, et al. LE135, a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels. Br J Pharmacol. 2014 Mar;171 (6) :1510-20.|[3]Y Li, et al. Identification of a novel class of retinoic acid receptor beta-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells. J Biol Chem. 1999 May 28;274 (22) :15360-6.