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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.74%
- CAS 番号: 188645-44-5
- 分子式: C33H32N2O2
- 分子量:488.62
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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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.
|
[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.
化学情報
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CAS 番号 188645-44-5
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性状 Solid
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分子量 488.62
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |