アピシジン
Based on 6 publication(s) in Google Scholar
Apicidin (OSI 2040) is a fungal metabolite, acts as an orally active histone deacetylase 7/8 (HDAC7/8) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity. Apicidin can be used for cancer research.
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: 99.49%
- CAS 番号: 183506-66-3
- 分子式: C34H49N5O6
- 分子量:623.78
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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RT-PCR
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Others
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生物活性
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HDAC7 |
HDAC8 |
Apicidin inhibits mammalian (HeLa) cell proliferation in vitro (50% inhibitory concentrations, 50-100 nM)[2].
Apicidin (0.1-10 μM, 24 h) inhibits the growth and the expression of HDAC in AT-84 cells dose-dependently[4].
Apicidin (1, 5 μM, 24 h) induces apoptosis and autophagy in AT-84 cells dose-dependently[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C mice[2].
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Dosage:2-20 mg/kg (i.p.); 25/50 mg/kg (oral).
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Administration:I.P. and Oral.
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Result:Demonstrated parenteral and oral efficacy against an acute strain of P. berghei in mice.
化学情報
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CAS 番号 183506-66-3
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性状 Solid
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分子量 623.78
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分子式 C34H49N5O6
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Color White to off-white
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SMILES
O=C(NC(C(N1[C@]2([H])CCCC1)=O)[C@@H](C)CC)[C@@H](NC([C@@H](NC2=O)CCCCCC(CC)=O)=O)CC3=CN(OC)C4=C3C=CC=C4
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別名
Apicidin; OSI 2040
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Structure Classification
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Initial Source
Toxic Fusarium
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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 In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Phosphatase LHPP confers prostate cancer ferroptosis activation by modulating the AKT-SKP2-ACSL4 pathway. [Abstract]2024 Sep 11;15(9):665. PMID: 39261475 -
Cancer Biol Ther
Apicidin confers promising therapeutic effect on acute myeloid leukemia cells via increasing QPCT expression. [Abstract]2023 Dec 31;24(1):2228497. PMID: 37381175
Apicidin purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2023 Dec 31;24(1):2228497. [Abstract]
THP-1 cells were treated with Apidin for 48–72 hours. Cell proliferation was then assessed using the CCK-8 assay.
Apicidin purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2023 Dec 31;24(1):2228497. [Abstract]
THP-1 cells were treated with Apidin for 48–72 hours. Apoptosis was analyzed by Annexin V and 7-AAD double staining combined with flow cytometry.
Apicidin purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2023 Dec 31;24(1):2228497. [Abstract]
The expression of QPCT protein in THP-1, NB4, and HL-60 cells treated with Apidin (1 μM) or DMSO for 48 hours was detected by Western blot.
Apicidin purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2023 Dec 31;24(1):2228497. [Abstract]
Qrt-PCR analysis was performed on the expression of QPCT in AML monocytes (MNCs) treated with Apidin (1 μM).
Apicidin purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2023 Dec 31;24(1):2228497. [Abstract]
Apicidin (1 μM) was used to detect the sonication efficiency of genomic DNA by agarose gel electrophoresis.
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FASEB J
GRK5 Overexpression Drives Malignant Glioma Progression Through HDAC7 Alongside Canonical GPCR Signaling. [Abstract]2026 Jan 31;40(2):e71475. PMID: 41553075 -
Vascular
Exploration of small molecule compounds targeting abdominal aortic aneurysm based on CMap database and molecular dynamics simulation. [Abstract]2024 Aug 18:17085381241273289. PMID: 39155144 -
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溶剤 & 溶解度
DMSO : 25 mg/mL (40.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (277 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Han JW, et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res. 2000 Nov 1;60(21):6068-74. [Content Brief]
[2]. S J Darkin-Rattray, et al. Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase. Proc Natl Acad Sci U S A. 1996 Nov 12;93(23):13143-7. [Content Brief]
[3]. Beom Soo Shin, et al. Quantitative determination of absorption and first-pass metabolism of apicidin, a potent histone deacetylase inhibitor. Drug Metab Dispos. 2014 Jun;42(6):974-82. [Content Brief]
[4]. Ahn MY, et al. HDAC inhibitor apicidin suppresses murine oral squamous cell carcinoma cell growth in vitro and in vivo via inhibiting HDAC8 expression. Oncol Lett. 2018 Nov;16(5):6552-6560. [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 | 1.6031 mL | 8.0156 mL | 16.0313 mL | 40.0782 mL |
| 5 mM | 0.3206 mL | 1.6031 mL | 3.2063 mL | 8.0156 mL | |
| 10 mM | 0.1603 mL | 0.8016 mL | 1.6031 mL | 4.0078 mL | |
| 15 mM | 0.1069 mL | 0.5344 mL | 1.0688 mL | 2.6719 mL | |
| 20 mM | 0.0802 mL | 0.4008 mL | 0.8016 mL | 2.0039 mL | |
| 25 mM | 0.0641 mL | 0.3206 mL | 0.6413 mL | 1.6031 mL | |
| 30 mM | 0.0534 mL | 0.2672 mL | 0.5344 mL | 1.3359 mL | |
| 40 mM | 0.0401 mL | 0.2004 mL | 0.4008 mL | 1.0020 mL |