2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. LE-540

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

For research use only. We do not sell to patients.

LE-540

LE-540 Chemical Structure

CAS No. : 188645-44-5

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LE-540 Related Antibodies

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RXRα RXRβ RXRγ

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Description

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

IC50 & Target

RXRβ

0.22 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
3.6 x 10-8M
Compound: 17
Concentration which reduces by half the percentage of differentiated HL-60 cells induced by 1 x 10e-9 M Am80.
Concentration which reduces by half the percentage of differentiated HL-60 cells induced by 1 x 10e-9 M Am80.
[PMID: 9435893]
In Vitro

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.

LE-540 Related Antibodies
Molecular Weight

488.62

Formula

C33H32N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (40.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0466 mL 10.2329 mL 20.4658 mL
5 mM 0.4093 mL 2.0466 mL 4.0932 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0466 mL 10.2329 mL 20.4658 mL 51.1645 mL
5 mM 0.4093 mL 2.0466 mL 4.0932 mL 10.2329 mL
10 mM 0.2047 mL 1.0233 mL 2.0466 mL 5.1165 mL
15 mM 0.1364 mL 0.6822 mL 1.3644 mL 3.4110 mL
20 mM 0.1023 mL 0.5116 mL 1.0233 mL 2.5582 mL
25 mM 0.0819 mL 0.4093 mL 0.8186 mL 2.0466 mL
30 mM 0.0682 mL 0.3411 mL 0.6822 mL 1.7055 mL
40 mM 0.0512 mL 0.2558 mL 0.5116 mL 1.2791 mL
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LE-540 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LE-540188645-44-5LE540LE 540RAR/RXRRetinoic acid receptorsRetinoid X receptorsα4β7 integrinRAR subtypeshippocampal neuronCCR9Sprague-Dawley ratretinoic acid receptorP-selectin ligandCD4+ T cellsT cellliver sinusoidal endothelial cellsInhibitorinhibitorinhibit

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