| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
SIRT5[1]
MC3482 targets sirtuin 5 (SIRT5). SIRT5 is a mitochondrial NAD⁺-dependent deacylase that removes acyl groups from lysine residues on proteins, regulating various metabolic pathways. By inhibiting SIRT5, MC3482 blocks its desuccinylating activity. This leads to increased ammonia content in cells, which triggers autophagy and mitophagy. |
|---|---|
| ln Vitro |
Inhibiting Sirtuin 5 is MC3482. SIRT5 desuccinylating activity is inhibited by 50 μM MC3482, although SIRT5 intracellular expression levels remain unchanged. In SIRT5-silenced cells and WT cells treated with MC3482, autophagy and mitophagy are upregulated, but they are downregulated in SIRT5-overexpressing cells[1].
In vitro, MC3482 inhibits SIRT5 desuccinylating activity. At 50 μM, MC3482 blocks SIRT5 activity without affecting its intracellular expression levels. In SIRT5-silenced cells and cells treated with MC3482, autophagy and mitophagy levels are increased. These in vitro activities support its use in studying SIRT5 biology, autophagy, and metabolism. |
| ln Vivo |
In vivo, MC3482 mitigates microglia-induced neuroinflammation and neuronal apoptosis by regulating Annexin-A1 succinylation. It significantly improves long-term sensorimotor and cognitive function, exhibiting potential for treating neuroinflammatory conditions. However, specific published in vivo efficacy studies for cancer are not detailed in the current literature.
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| Enzyme Assay |
The in vitro SIRT5 inhibition assay for MC3482 uses recombinant SIRT5 enzyme and a fluorogenic peptide substrate. Enzyme activity is measured by quantifying the deacylation of the substrate. The compound is added at various concentrations, and IC50 values are calculated from dose-response curves. Selectivity profiling against other sirtuins (SIRT1-3) is performed to confirm specificity.
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| Cell Assay |
Cellular assays for MC3482 are conducted in various cell lines. Cells are treated with varying concentrations of MC3482. SIRT5 activity is measured in cell lysates using activity assays. Autophagy and mitophagy are assessed by monitoring LC3-II accumulation and mitochondrial markers using Western blotting and fluorescence microscopy. Cell viability is measured using standard assays.
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| Animal Protocol |
In vivo studies for MC3482 are conducted in mouse models of neuroinflammation. The compound is administered via oral or intraperitoneal routes. Efficacy is assessed by measuring neuroinflammation markers, neuronal apoptosis, and cognitive function. However, specific published in vivo protocols for MC3482 are not detailed in the available literature. The compound is used in research on neuroinflammation and cancer.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MC3482 is not extensively reported in publicly available sources. The compound has a molecular weight of 618.68 and a molecular formula of C33H38N4O8. It has a CAS number of 2922280-86-0. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for MC3482 is limited. As with all research compounds, MC3482 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
MC3482 (CAS 2922280-86-0) is a potent, specific, and cell-permeable inhibitor of sirtuin 5 (SIRT5). It increases ammonia content in cells, leading to autophagy and mitophagy. MC3482 mitigates microglia-induced neuroinflammation and neuronal apoptosis. It has a molecular formula of C33H38N4O8 and a molecular weight of 618.68. It is for research use only.
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| Molecular Formula |
C33H38N4O8
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|---|---|
| Molecular Weight |
618.676828861237
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| Exact Mass |
618.268
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| CAS # |
2922280-86-0
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| PubChem CID |
134694957
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
45
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| Complexity |
930
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1=CC=C(C=C1)COC(=O)N[C@@H](CCCCNC(=O)CC[C@@H](C(=O)O)NC(=O)OCC2=CC=CC=C2)C(=O)NC3=CC=CC=C3
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| InChi Key |
LDCYHYVNYRUUOL-NSOVKSMOSA-N
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| InChi Code |
InChI=1S/C33H38N4O8/c38-29(20-19-28(31(40)41)37-33(43)45-23-25-14-6-2-7-15-25)34-21-11-10-18-27(30(39)35-26-16-8-3-9-17-26)36-32(42)44-22-24-12-4-1-5-13-24/h1-9,12-17,27-28H,10-11,18-23H2,(H,34,38)(H,35,39)(H,36,42)(H,37,43)(H,40,41)/t27-,28-/m0/s1
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| Chemical Name |
(2S)-5-[[(5S)-6-anilino-6-oxo-5-(phenylmethoxycarbonylamino)hexyl]amino]-5-oxo-2-(phenylmethoxycarbonylamino)pentanoic acid
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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 : ≥ 130 mg/mL (210.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6163 mL | 8.0817 mL | 16.1634 mL | |
| 5 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL | |
| 10 mM | 0.1616 mL | 0.8082 mL | 1.6163 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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