A RAR antagonist with moderate selectivity for RARβ over RARα (Kis = 0.22 and 1.4 μM

LE 135 – 5 mg

Brand:
Cayman
CAS:
155877-83-1
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A RAR antagonist with moderate selectivity for RARβ over RARα (Kis = 0.22 and 1.4 μM, respectively); inhibits retinoid Am80-induced differentiatiobn of HL-60 cells (IC50 = 0.2 μM)

Formal 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

Synonyms: 

Molecular weight: 438.6

CAS: 155877-83-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs

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