LE 135

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LE 135

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Cat No: 14415

Biochemicals - Receptor Pharmacology

LE 135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (Kis = 0.22 and 1.4 μM, respectively).{23265,23266} LE 135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

retinoic acids receptors RARs antagonists RAR? transcriptions activations inhibitors inhibits inhibitions LE135 LE-135 Les 135 RARb RAR-b b RAR.beta. RAR-.beta. .beta. RARbeta RAR-beta beta RAR-? ? acid-induced induces transcriptional RXRs RXRa RXR-a RXRalpha RXR-alpha RXR.alpha. RXR-.alpha. RXR? ? retinoids am80 am-80 ams 80 80-induced humans leukemia HL-60 HL60 HLs 60 cells promyelocytic nuclears receptors biology cancers moderate selectivity RAR? RARgamma RAR.gamma. RAR-gamma RARg RAR-g g X alpha beta gamma ? differentiations

Product Overview:
LE 135 is a retinoic acid receptor (RAR) antagonist that displays moderate selectivity for RARβ over RARα (Kis = 0.22 and 1.4 μM, respectively).{23265,23266} LE 135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α.{23265} It has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia cells, HL-60, with an IC50 value of 0.2 μM.{23076}

Size	1 mg
Shipping	dry ice
CAS Number	155877-83-1
Molecular Formula	C₂₉H₃₀N₂O₂
SMILES	CC1(C)C2=C(C=C(N(C)C(C=CC=C3)=C3C(C4=CC=C(C(O)=O)C=C4)=N5)C5=C2)C(C)(C)CC1
Molecular Weight	438,6
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.