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LE135

Catalog No. T22920 CAS 155877-83-1

Synonyms: LE 135

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.

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LE135, CAS 155877-83-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 56.00
5 mg	In stock	$ 93.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 342.00
100 mg	In stock	$ 497.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.33%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	RARβ:220 nM (Ki), TRPV1:2.5 μM (EC50), TRPA1:20 μM (EC50), RARα:1400 nM (Ki)
In vitro	LE135 blocks the differentiation of human promyelocytic leukemia cells HL-60, triggered by Am80, with an inhibitory concentration (IC50) of 150 nM. It specifically hinders retinoic acid (RA)-prompted transcriptional activation of the retinoic acid receptor beta (RARβ) without affecting RARα, RARγ, or the retinoid X receptor alpha (RXRα) across various RA response elements. Furthermore, LE135 significantly suppresses the activity of the AP-1 transcription factor induced by 12-O-tetradecanoylphorbol-13-acetate in cells that express RARβ and RXRα.
In vivo	LE135 induces nociceptive responses and thermal hyperalgesia primarily via TRPV1 channels, and necessitates both TRPA1 and TRPV1 channels to cause mechanical allodynia. Intraplantar injection of LE135 (30 nmol/10 μL) results in mechanical hypersensitivity in both wild-type and Trpa1−/− mice[2].

Synonyms	LE 135
Molecular Weight	438.56
Formula	C29H30N2O2
CAS No.	155877-83-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (102.6 mM), Sonication is recommended.

References and Literature

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):15

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Neuronal Differentiation Compound Library Nuclear Receptor Compound Library

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Keywords

LE135 155877-83-1 Metabolism Retinoid Receptor LE-135 LE 135 inhibitor inhibit

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