MN 64 |
Catalog No.GC16914
One-Click Copy Product Info
|
tankyrase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 92831-11-3
Sample solution is provided at 25 µL, 10mM.
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MN-64 is a type of flavone that act as a potent and selective tankyrase inhibitor (IC50 = 6 and 72 nM for TNKS1 and TNKS2, respectively). [1]
Tankytase (TNKS) is a member of poly ADP ribose polymerases (PARPs). There are two related homologue, TNKS1 and TNKS2 that are mostly located in the nuclear pore, cytoplasm, mitotic centrosomes and the Golgi apparatus. They involve in cellular functions such as regulation of cell proliferation and promoting telomere elongation in human cells. [1]
During an assay for screening flavone TNKS inhibitors, MN-64 is discovered for abrogating STF luciferase activity at 200nM and potently inhibiting TNKS1 with IC50 of 6nM. It also selectively inhibits TNKS1 and TNKS2 without affecting any other PARPs. Moreover, MN-64 is prominently more selective than other TNKS inhibitors such as XAV939. [1]
Reference:
1. Narwal M, Koivunen J, Haikarainen T et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9.
Kinase experiment: | Inhibitory potency of compounds on Tankyrase-1 enzymatic activity is evaluated using a Scintillation Proximity Assay (SPA). The assay is designed to measure compound inhibition of Tankyrase-1 autoPARsylation (Tankyrase-1 is both enzyme and substrate in this assay). Truncated recombinant human Tankyrase-1 protein (amino acids E1023-T1327) is purified from SF9 cells. The assay is conducted using 0.11 μM of Tankyrase-1 protein and 3 μM nicotinamide adenine dinucleotide (NAD+, 2.12 μM 3H-NAD+ with a specific radioactivity of 1690 Ci/mol, 0.88 μM biotin- NAD+), in pH 7.5 Tris buffer (60 mM Tris, 1 mM DTT, 0.01% (v/v) Tween-20®, 2.5 mM MgCl2, 0.3 mg/mL BSA). For IC50 determination, 10 mM DMSO stock solution of a compound (MN-64) is sequentially diluted by two-fold in DMSO, and aliquots of the diluted solutions are transferred to 384-well assay plates and mixed with Tankyrase-1 solution[1]. |
References: [1]. Narwal M, et al. Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9. | |
| Cas No. | 92831-11-3 | SDF | |
| Chemical Name | 2-(4-isopropylphenyl)-4H-chromen-4-one | ||
| Canonical SMILES | CC(C1=CC=C(C2=CC(C3=CC=CC=C3O2)=O)C=C1)C | ||
| Formula | C18H16O2 | M.Wt | 264.32 |
| Solubility | ≥ 11.65mg/mL in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7833 mL | 18.9165 mL | 37.8329 mL |
| 5 mM | 756.7 μL | 3.7833 mL | 7.5666 mL |
| 10 mM | 378.3 μL | 1.8916 mL | 3.7833 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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)