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LE 135

SIGMA/SML0809 - ≥98% (HPLC)

Synonym: 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; LE-135

CAS Number: 155877-83-1
Empirical Formula (Hill Notation): C29H30N2O2
Molecular Weight: 438.56
Linear Formula: C29H30N2O2
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML0809-5MG 5 mg
 $111.00
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45-SML0809-25MG 25 mg
 $448.00
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This image is provided for informative purposes only and does not represent an actual product label. It should not be used as a substitute for official product labeling.

 

assay ≥98% (HPLC)
color yellow to orange
form powder
InChI 1S/C29H30N2O2/c1-28(2)14-15-29(3,4)22-17-25-23(16-21(22)28)30-26(18-10-12-19(13-11-18)27(32)33)20-8-6-7-9-24(20)31(25)5/h6-13,16-17H,14-15H2,1-5H3,(H,32,33)
InChI key YZZAIQOVMHVWBS-UHFFFAOYSA-N
Quality Level 100 
SMILES string N1(c2c(cc5c(c2)C(CCC5(C)C)(C)C)N=C(c4c1cccc4)c3ccc(cc3)C(=O)O)C
solubility DMSO: 15 mg/mL, clear
storage temp. 2-8°C
Application: LE 135 has been used for in vitro islet treatment.
Biochem/physiol Actions: LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM).
Biochem/physiol Actions: LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC50 value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.
Features and Benefits: This compound is featured on the Nuclear Receptors (Non-Steroids)  page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here .
Packaging: 5, 25 mg in glass bottle
Symbol GHS07  GHS07
Signal word Warning
Hazard statements H315 - H319
Precautionary statements P302 + P352 - P305 + P351 + P338
Hazard Codes Xi
Risk Statements 36/38
Safety Statements 26
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352200

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