LE-540 

LE-540 is a selective retinoic acid receptor antagonist for RARβ (K_i=0.22 μM). LE-540 shows potential for use in cancer research, particularly for breast cancer and lung cancer^[1][2].

LE-540 (10^-7 M; 3 days) does not block the negative effects of 10^-4 M 13-cis-RA on primary cultured embryonic day 21 Sprague-Dawley rat hippocampal neuron survival or dendritic morphology^[1].
LE-540 (10^-9-10^-7 M; 3 days) blocks the negative effects of 10^-6 M all-trans-RA on primary cultured embryonic day 21 Sprague-Dawley rat hippocampal neuron survival and dendritic morphology, with 10^-7 M LE-540 showing synergistic effects on neuron number when combined with 10^-6 M all-trans-RA^[1].
LE-540 (10^-11 M; 3 days) is more potent than higher concentrations (10^-9 M, 10^-7 M) at blocking the positive effects of 10^-8 M 13-cis-RA on primary cultured embryonic day 21 Sprague-Dawley rat hippocampal neuron survival and dendritic morphology^[1].
LE-540 (10^-8 M; 3 days) specifically blocks the negative effects of 10^-6 M 9-cis-RA on primary cultured embryonic day 21 Sprague-Dawley rat hippocampal neuron survival and dendritic morphology, while lower (10^-10 M) and higher (10^-6 M) concentrations do not^[1].
LE-540 (10^-11-10^-7 M; 3 days) has no independent effect on primary cultured embryonic day 21 Sprague-Dawley rat hippocampal neuron survival or dendritic morphology^[1].
LE-540 (1 μM; 6 days) blocks RAR signaling in LSEC-primed naive CD4⁺ T cells, eliminating induction of gut-homing molecules α₄β₇ integrin and CCR9 while increasing expression of skin/inflammation-homing P-lig^[2].
LE-540 (1 μM; 6 days) abolishes functional CCR9-mediated transmigration of LSEC-primed CD4⁺ T cells toward CCL25^[2].
LE-540 (1 μM; 6 days) blocks RAR signaling in LSEC-primed CD8⁺ T cells, reducing induction of gut-homing molecules α₄β₇ integrin and CCR9 while increasing expression of skin/inflammation-homing P-lig^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

488.62

C₃₃H₃₂N₂O₂

188645-44-5

O=C(O)C1=CC=C(C2=NC3=CC4=C(C(C)(C)CCC4(C)C)C=C3N(C)C5=C6C=CC=CC6=CC=C52)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu Y, et al. Effects of retinoic acids on the dendritic morphology of cultured hippocampal neurons. J Neurochem. 2008;106(3):1104-1116.  [Content Brief]

  [2]. Neumann K, et al. Connecting liver and gut: murine liver sinusoidal endothelium induces gut tropism of CD4+ T cells via retinoic acid. Hepatology. 2012 Jun;55(6):1976-84.  [Content Brief]