Apicidin (Synonyms: OSI 2040) |
| Catalog No.GC12961 |
A cell-permeable HDAC inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 183506-66-3
Sample solution is provided at 25 µL, 10mM.
Histone acetyltransferase and histone deacetylase (HDAC) activity regulates the reversible acetylation of lysine residues within histone tails, which results in either transcriptional activation or repression of nearby genes. Compounds that modulate this activity are of interest in cancer chemotherapeutics as well as for treating psychiatric disorders, malaria, and other diseases. Apicidin is a fungal toxin that has broad spectrum activity against Apicomplexan parasites through inhibiting HDACs (IC50 = 0.7 nM).[1] An in vitro activity assay demonstrates apicidin inhibition of HDAC3/NCoR, a class I HDAC, at a much higher potency than for class II HDAC6 (IC50s = 15.8 and 665.1 nM, respectively).[2] Apicidin exhibits antiproliferative activity against various cancer cell lines (IC50s = 0.13-2.36 μM), and at 0.5 – 2 μM it induces selective changes in p21WAF1/Cip1 and gelsolin gene expression, which control cell cycle and cell morphology, respectively.[3]
Reference:
[1]. Darkin-Rattray, S.J., Gurnett, A.M., Myers, R.W., et al. Apicidin: A novel antiprotozoal agent that inhibits parasite histone deacetylase. Proceedings of the National Academy of Sciences of the United States of America 93(23), 13143-13147 (1996).
[2]. Mazitschek, R., Patel, V., Wirth, D.F., et al. Development of a fluorescence polarization based assay for histone deacetylase ligand discovery. Bioorg. Med. Chem. Lett. 18(9), 2809-2812 (2008).
[3]. Han, J.W., Ahn, S.H., Park, S.H., et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Research 60, 6068-6074 (2000).
| Cell experiment [1]: | |
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Cell lines |
HeLa cells |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
1 μg/mL; 24 hrs |
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Applications |
Apicidin exhibited long-lasting anti-proliferative activity against HeLa cells, up to 48 hrs after withdrawal. |
| Animal experiment [2]: | |
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Animal models |
Ishikawa endometrial cancer xenografted mouse model |
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Dosage form |
5 mg/kg; i.p.; q.d., for 21 days |
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Applications |
Significant inhibition of tumor growth was observed starting from day 15 after the Apicidin treatment. Apicidin (5 mg/kg) significantly inhibited tumor growth up to 53%. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Han JW, Ahn SH, Park SH, Wang SY, Bae GU, Seo DW, et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res 2000,60:6068-6074. [2]. Ahn MY, Chung HY, Choi WS, Lee BM, Yoon S, Kim HS. Anti-tumor effect of apicidin on Ishikawa human endometrial cancer cells both in vitro and in vivo by blocking histone deacetylase 3 and 4. Int J Oncol 2010,36:125-131. |
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| Cas No. | 183506-66-3 | SDF | |
| Synonyms | OSI 2040 | ||
| Chemical Name | (3S,6S,9S,12R)-3-[(2S)-butan-2-yl]-6-[(1-methoxyindol-3-yl)methyl]-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone | ||
| Canonical SMILES | CCC(C)C1C(=O)N2CCCCC2C(=O)NC(C(=O)NC(C(=O)N1)CC3=CN(C4=CC=CC=C43)OC)CCCCCC(=O)CC | ||
| Formula | C34H49N5O6 | M.Wt | 623.78 |
| Solubility | 1mg/mL in DMSO or acetonitrile | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6031 mL | 8.0156 mL | 16.0313 mL |
| 5 mM | 0.3206 mL | 1.6031 mL | 3.2063 mL |
| 10 mM | 0.1603 mL | 0.8016 mL | 1.6031 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
Apicidin treatment relieves Aβ plaques in APP/PS1 mice. (A) Representative immunohistochemical images of 6E10-labeled Aβ burden in the coronal and hippocampal sections of AD-ap and AD-ns mice.
Apicidin (GLPBIO) was dissolved in 5% Tween 80 to generate a 20 mM stock solution and stored at −80°C.
Cns Neurosci Ther (2023). PMID: 36708130 IF: 7.0348 -
Related Biological Data
Effect of lactylation on cell migration and proliferation in HCC. A CCK-8 assay showed the cell proliferation ability of LM3 (G) and Huh7 (H) cultured by 0, 1, or 2 μM of apicidin for 48 h.
Using the TRIzol method, total RNA was extracted from LM3 and Huh7 after being treated with 0 μM and 1 μM of apicidin (GLPBIO), respectively, for 48 h.
J Cancer Res Clin (2023): 1-14. PMID: 37400571 IF: 3.5999
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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