LE 135

Name: LE 135
Brand: Tocris Bioscience
SKU: 2021

Tocris Bioscience, part of Bio-Techne | Catalog # 2021

Citations (289)

COA / SDS

Selective RARβ antagonist

Key Product Details

Description:	Selective RARβ antagonist
Chemical Name:	4-(7,8,9,10-Tetrahydro-5,7,7,10,10-pentamethyl-5H-benzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid
Purity:	≥97% (HPLC)
Molecular Weight:	438.56

View Full Technical Details for LE 135

Technical Data
Citations

Biological Activity for LE 135

LE 135 is a retinoic acid antagonist; displays moderate selectivity for RARβ over RARα (K_i values are 0.22 and 1.4 μM respectively). Highly selective over RARγ and RXRα. Inhibits human HL-60 leukemia cell differentiation induced by Am80 (IC₅₀ = 150 nM).

Technical Data for LE 135

M. Wt	438.56
Formula	C₂₉H₃₀N₂O₂
Storage	Store at +4°C
Purity	≥97% (HPLC)
CAS Number	155877-83-1
PubChem ID	10410894
InChi Key	YZZAIQOVMHVWBS-UHFFFAOYSA-N
Smiles	CN1C2=C(C=C3C(=C2)C(C)(C)CCC3(C)C)N=C(C2=CC=C(C=C2)C(O)=O)C2=C1C=CC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for LE 135

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	43.86	100

Preparing Stock Solutions for LE 135

The following data is based on the product molecular weight 438.56.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.28 mL	11.40 mL	22.80 mL
5 mM	0.46 mL	2.28 mL	4.56 mL
10 mM	0.23 mL	1.14 mL	2.28 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References for LE 135

References are publications that support the biological activity of the product.

Umemiya Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J.Med.Chem. 1997 PMID: 9435893
Li Identification of a novel class of retinoic acid receptor β-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 PMID: 10336422
Eyrolles Retinobenzoic acids. 6. Retinoid antagonists with heterocyclic ring. J.Med.Chem. 1994 PMID: 8182710