| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H16O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
MN-64 inhibits tankyrase 1, with IC50 values of 6 nM for TNKS1, 72 nM for TNKS2, 19.1 μM for ARTD1, and 39.4 μM for ARTD2. It is supplied as a light yellow to yellow solid (C18H16O2, MW 264.32) at 99.61% purity.
Physical & Chemical Properties
| CAS Number | 92831-11-3 |
|---|---|
| Molecular Formula | C18H16O2 |
| Molecular Weight | 264.32 g/mol |
| Purity | 99.61% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C1C=C(C2=CC=C(C(C)C)C=C2)OC3=CC=CC=C13 |
| Target | TNKS1, TNKS2, ARTD1, ARTD2 |
| Signaling Pathway | Cell Cycle/DNA Damage; Epigenetics |
| Solubility | In Vitro: DMSO: 100 mg/mL (378.33 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
TNKS1 6 nM (IC50) |
TNKS2 72 nM (IC50) |
ARTD1 19.1 μM (IC50) |
ARTD2 39.4 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (378.33 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (9.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (9.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (9.46 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
MN-64 inhibits tankyrase 1 potently, with IC50s of 6 nM for TNKS1, 72 nM for TNKS2, 19.1 μM for ARTD1, and 39.4 μM for ARTD2. At 1 μM, MN-64 effectively inhibits Wnt/β-catenin, and at 200 nM it blocks STF luciferase activity[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Evaluate the inhibitory potency of compounds on Tankyrase-1 enzymatic activity with a Scintillation Proximity Assay (SPA), which measures compound inhibition of Tankyrase-1 autoPARsylation (Tankyrase-1 serves as both enzyme and substrate). Purify truncated recombinant human Tankyrase-1 protein (amino acids E1023-T1327) from SF9 cells. Run the assay with Tankyrase-1 protein at 0.11 μM and 3 μM NAD+ (nicotinamide adenine dinucleotide), including 2.12 μM 3H-NAD+ (specific radioactivity of 1690 Ci/mol) and 0.88 μM biotin- NAD+, in Tris buffer, pH 7.5, containing 60 mM Tris, 1 mM DTT, 2.5 mM MgCl2, 0.01% (v/v) Tween-20®, and 0.3 mg/mL BSA. For IC50 determination, dilute a 10 mM DMSO stock solution of the compound (MN-64) sequentially by two-fold in DMSO, transfer aliquots of the diluted solutions to 384-well assay plates, and mix with Tankyrase-1 solution[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Tankyrase inhibition preserves osteoarthritic cartilage by coordinating cartilage matrix anabolism via effects on SOX9 PARylation. Nat Commun 2019 Oct 25;10(1):4898.
Combination of PARP inhibitor and temozolomide to suppress chordoma progression. J Mol Med (Berl) 2019 Aug;97(8):1183-1193.
Patent. US20210353681A1.
PMID: 31653858
