| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
HDAC
Apicidin targets histone deacetylases (HDACs), a family of enzymes that remove acetyl groups from histone proteins. It has been shown to inhibit HDAC1, HDAC2, HDAC3, HDAC7, and HDAC8. By inhibiting these enzymes, apicidin promotes a more open chromatin structure, which can lead to the re-expression of tumor suppressor genes and the induction of cell cycle arrest and apoptosis. |
|---|---|
| ln Vitro |
In vitro, apicidin inhibits tumor cell proliferation through gene expression changes of p21WAF1/Cip1 and gelsolin, and can cause cell cycle arrest in the G1 phase. It dramatically decreases HIF-1α protein levels and transcriptional activity in human and mouse tumor cell lines. It induces morphological changes, cell cycle arrest at G1 phase, and accumulation of hyperacetylated histone H4 in HeLa cells.
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| ln Vivo |
In vivo, apicidin reduces Aβ load and alleviates memory deficits in APP/PS1 mice. It inhibits cell growth and proliferation, induces apoptosis and autophagy, and has been studied for the treatment of leukemia. Its antiparasitic activity has also been demonstrated in vivo. However, specific details of in vivo studies are not extensively detailed in the available literature.
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| Enzyme Assay |
The in vitro enzyme assay for apicidin measures its ability to inhibit HDAC activity. These cell-free assays use purified HDAC enzymes and a fluorogenic or radiolabeled substrate. The compound's inhibitory potency (IC50) is determined by measuring the reduction in deacetylase activity. These assays provide a direct measure of the compound's potency against specific HDAC isoforms.
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| Cell Assay |
In vitro cellular assays for apicidin assess its effects on histone acetylation and gene expression. Cells are treated with apicidin, and histone acetylation levels are measured by Western blot. Cell cycle analysis is performed using flow cytometry, and apoptosis is assessed using Annexin V staining or caspase activity assays. These assays demonstrate the compound's functional activity as an HDAC inhibitor in a cellular context.
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| Animal Protocol |
In vivo animal studies for apicidin have been conducted in mouse models to evaluate its efficacy. In APP/PS1 mice, it reduced Aβ load and alleviated memory deficits. Its effects on tumor growth have also been studied in xenograft models. These studies demonstrate the compound's in vivo activity and potential therapeutic applications.
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| ADME/Pharmacokinetics |
Apicidin is orally active. Its pharmacokinetic properties support oral administration. As a small molecule HDAC inhibitor, it is absorbed and distributed throughout the body. However, detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively detailed in the available literature. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for apicidin are not extensively detailed in the available literature. As an HDAC inhibitor, its toxicity profile is likely related to its mechanism of action. However, its in vivo efficacy at tolerable doses has been demonstrated. It is intended for research purposes only and is not for human use.
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| References | |
| Additional Infomation |
Apicidin is a fungal metabolite and a potent HDAC inhibitor with antiparasitic and antiproliferative activities. It is a valuable research tool for studying the role of HDACs in gene expression, cell cycle regulation, and cancer. It is not approved for clinical use and is intended for research purposes only.
|
| Molecular Formula |
C34H49N5O6
|
|---|---|
| Molecular Weight |
623.78
|
| Exact Mass |
609.353
|
| Elemental Analysis |
C, 65.47; H, 7.92; N, 11.23; O, 15.39
|
| CAS # |
183506-66-3
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| Related CAS # |
183506-66-3
|
| PubChem CID |
6918328
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| Appearance |
Solid powder
|
| Density |
1.27g/cm3
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| Index of Refraction |
1.615
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| LogP |
4.121
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
45
|
| Complexity |
1050
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
C1CN2C(=O)[C@H](C(C)CC)NC(=O)[C@H](CC3=CN(OC)C4C=CC=CC3=4)NC(=O)[C@H](CCCCCC(=O)CC)NC(=O)[C@H]2CC1
|
| InChi Key |
ROUDRKBLRFRFCY-VWIQTCEGSA-N
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| InChi Code |
InChI=1S/C34H49N5O6/c1-5-22(3)30-34(44)38-19-13-12-18-29(38)33(43)35-26(16-9-7-8-15-25(40)6-2)31(41)36-27(32(42)37-30)21-24-20-23-14-10-11-17-28(23)39(24)45-4/h10-11,14,17,20,22,26-27,29-30H,5-9,12-13,15-16,18-19,21H2,1-4H3,(H,35,43)(H,36,41)(H,37,42)/t22-,26+,27+,29-,30+/m1/s1
|
| Chemical Name |
(3S,6S,9S,15aR)-9-((R)-sec-butyl)-6-((1-methoxy-1H-indol-2-yl)methyl)-3-(6-oxooctyl)decahydro-1H-pyrido[1,2-a][1,4,7,10]tetraazacyclododecine-1,4,7,10(12H)-tetraone
|
| Synonyms |
Apicidin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~25 mg/mL (~40.1 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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