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
assay |
≥98% (HPLC) |
color |
yellow to orange |
form |
powder |
Quality Level |
100 |
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). 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 |
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 |