LE-540
Based on 1 Customer Validation
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.
- Purity: 99.74%
- CAS No.: 188645-44-5
- Formula: C33H32N2O2
- Molecular Weight:488.62
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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RXRβ 0.22 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
3.6 x 10-8M
Compound: 17
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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.
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[PMID: 9435893] |
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.
Chemical Information
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CAS No. 188645-44-5
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Appearance Solid
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Molecular Weight 488.62
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Formula C33H32N2O2
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Color Light yellow to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (204.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[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]
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 | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4093 mL | 1.0233 mL | |
| 60 mM | 0.0341 mL | 0.1705 mL | 0.3411 mL | 0.8527 mL | |
| 80 mM | 0.0256 mL | 0.1279 mL | 0.2558 mL | 0.6396 mL | |
| 100 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5116 mL |
LE-540 Related Classifications
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