155877-83-1 Usage
Description
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). LE 135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α. 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.
Uses
LE 135 has been used for in vitro islet treatment.
Biological Activity
Retinoic acid antagonist; displays moderate selectivity for RAR β over RAR α (Ki values are 0.22 and 1.4 μ M respectively). Highly selective over RAR γ and RXR α . Inhibits human HL-60 leukemia cell differentiation induced by Am80 (IC 50 = 150 nM).
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.
Check Digit Verification of cas no
The CAS Registry Mumber 155877-83-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,5,8,7 and 7 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 155877-83:
(8*1)+(7*5)+(6*5)+(5*8)+(4*7)+(3*7)+(2*8)+(1*3)=181
181 % 10 = 1
So 155877-83-1 is a valid CAS Registry Number.
InChI:InChI=1/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)
155877-83-1Relevant articles and documents
Retinobenzoic Acids. 6. Retinoid Antagonists with a Heterocyclic Ring
Eyrolles, Laurence,Kagechika, Hiroyuki,Kawachi, Emiko,Fukasawa, Hiroshi,Iijima, Tohru,et al.
, p. 1508 - 1517 (1994)
Several candidate retinoid anatgonists were designed on the basis of the ligand superfamily concept and synthesized.Retinoidal activities of these benzimidazole and benzodiazepine derivatives were examined by assay of differentiation-inducing activity on