| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
mHTT-LC3 Linker Compound
LC3-mHTT-IN-AN2 targets mutant huntingtin protein (mHTT), the protein responsible for Huntington's disease, and LC3B, a key component of the autophagy machinery. As a "linker" compound, it simultaneously binds to mHTT and LC3B, thereby recruiting mHTT to autophagosomes for degradation. This mechanism allows for the selective clearance of the pathogenic mutant protein while sparing the wild-type huntingtin protein. |
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| ln Vitro |
In cultured HD mouse neurons, LC3-mHTT-IN-AN2 (10, 50, 100, and 300 nM) selectively lowers the levels of mHTT[1].
In vitro, LC3-mHTT-IN-AN2 interacts with both mutant huntingtin protein (mHTT) and LC3B, but not with wtHTT or irrelevant control proteins. It reduces mHTT levels in an allele-selective manner in cultured Huntington disease mouse neurons. The compound is found in Passiflora serratodigitata and has antibacterial activity. These in vitro activities support its use in studying Huntington disease and autophagy-targeted protein degradation. |
| ln Vivo |
In vivo data for LC3-mHTT-IN-AN2 is limited in publicly available sources. As a compound that selectively reduces mHTT levels in cultured Huntington disease mouse neurons, it has potential applications in animal models of Huntington's disease. By targeting mHTT for autophagic degradation, LC3-mHTT-IN-AN2 could alleviate the toxic effects of the mutant protein. However, specific published in vivo efficacy studies are not detailed in the current literature. LC3-mHTT-IN-AN2 is primarily used as a research tool for studying Huntington disease and autophagy.
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| Enzyme Assay |
The in vitro mHTT-LC3 interaction assay for LC3-mHTT-IN-AN2 uses purified mHTT and LC3B proteins. The compound's ability to bridge the two proteins is assessed using co-immunoprecipitation, pull-down assays, or fluorescence-based methods. mHTT levels are measured by Western blotting in cultured Huntington disease mouse neurons treated with the compound. Selectivity for mHTT over wtHTT is confirmed by comparing the effects on both proteins.
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| Cell Assay |
Cellular assays for LC3-mHTT-IN-AN2 are conducted in cultured Huntington disease mouse neurons. Cells are treated with varying concentrations of LC3-mHTT-IN-AN2. mHTT and wtHTT levels are measured by Western blotting. Autophagy activation is assessed by monitoring LC3-II accumulation and autophagosome formation using fluorescence microscopy. Cell viability is measured using standard assays. The compound's selectivity for mHTT over wtHTT is confirmed by comparing protein levels.
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| Animal Protocol |
In vivo studies for LC3-mHTT-IN-AN2 would typically involve mouse models of Huntington's disease. The compound would be administered via intraperitoneal or oral routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring mHTT levels in brain tissues, behavioral outcomes, and neuropathological markers. However, specific published in vivo protocols for LC3-mHTT-IN-AN2 are not available in the current literature. The compound is currently used as a research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for LC3-mHTT-IN-AN2 is not extensively reported in publicly available sources. The compound has a molecular weight of 254.24 g/mol and a molecular formula of C15H10O4. It has a CAS number of 7758-73-8. It is soluble in DMSO at 50 mg/mL. Storage: powder at -20°C for 3 years. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for LC3-mHTT-IN-AN2 is limited in publicly available sources. The compound is found in Passiflora serratodigitata and has antibacterial activity. As with all research compounds, LC3-mHTT-IN-AN2 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 |
Serratin is a novel flavonoid compound.
It has been reported that 5,7-dihydroxy-4-phenylcoumarin has been found in passion fruit (Passiflora serratodigitata), and relevant data are available for reference. LC3-mHTT-IN-AN2 (Compound AN2; CAS 7758-73-8) is a mHTT-LC3 linker compound that interacts with mutant huntingtin (mHTT) and LC3B, but not with wild-type huntingtin. It targets mHTT to autophagosomes, reducing mHTT levels in Huntington disease mouse neurons. It is also known as 5,7-Dihydroxy-4-phenylcoumarin and is found in Passiflora plants. LC3-mHTT-IN-AN2 has a molecular formula of C15H10O4 and a molecular weight of 254.24 g/mol. |
| Molecular Formula |
C15H10O4
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|---|---|
| Molecular Weight |
254.24
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| Exact Mass |
254.058
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| CAS # |
7758-73-8
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| PubChem CID |
5398649
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.443g/cm3
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| Boiling Point |
535.5ºC at 760mmHg
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| Melting Point |
227-233ºC(lit.)
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| Flash Point |
210.5ºC
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| LogP |
2.871
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
384
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HUQKUJNSVHEHIH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O4/c16-10-6-12(17)15-11(9-4-2-1-3-5-9)8-14(18)19-13(15)7-10/h1-8,16-17H
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| Chemical Name |
5,7-dihydroxy-4-phenylchromen-2-one
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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 : 125 mg/mL (491.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.18 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 20.8 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: ≥ 2.08 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL | |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL | |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 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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