| Size | Price | Stock | Qty |
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| Targets |
MRT59 targets CK1 (casein kinase 1) and CHK1 (checkpoint kinase 1). CK1 is a serine/threonine kinase involved in various cellular processes, including Wnt signaling, circadian rhythm, and DNA repair. CHK1 is a serine/threonine kinase that plays a critical role in the DNA damage response and cell cycle checkpoint control. MRT59 is a potent broad-spectrum kinase inhibitor with IC₅₀ values of 0.9 µM for CK1δ and 0.23 µM for CHK1. By inhibiting CK1 and CHK1, MRT59 induces p53 pathway activation and E2F-1 destabilisation. The compound is a valuable tool for studying cell cycle regulation and DNA damage response.
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| ln Vitro |
At 5 µM, MRT00033659 (5–40 µM; 48 hours) is enough to drastically lower the number of cells [1]. Massive cell death is induced by MRT00033659 (1-80 µM; 48 hours) beginning at 5 µM [1]. MRT00033659 (0.2-80 µM; 48 hours) destabilizes E2F-1 from 0.2 µM to 5 µM and produces steady and prolonged stabilization of p53, MDM2, and p21 proteins [1]. p38α MAPK is not inhibited by MRT00033659[1].
In vitro, MRT59 inhibits CK1 and CHK1 kinase activity in cell-free assays. In cell-based assays, MRT59 induces p53 pathway activation and E2F-1 destabilisation. The compound's activity is typically assessed by measuring the phosphorylation of CK1 and CHK1 substrates, as well as the expression of p53 target genes. MRT59 shows potent inhibitory activity against CK1δ (IC₅₀ = 0.9 µM) and CHK1 (IC₅₀ = 0.23 µM). The compound has pharmacological similarities to the CK1-inhibitor D4476 and the MDM2-inhibitor Nutlin-3. |
| ln Vivo |
In vivo, MRT59 has been studied for its potential anticancer effects. As a CK1 and CHK1 inhibitor, it is expected to induce cell cycle arrest and apoptosis in cancer cells. The compound's ability to activate the p53 pathway may contribute to its antitumor activity. Specific in vivo efficacy data are limited in the published literature. MRT59 is a research tool for studying CK1 and CHK1 biology and their roles in cancer.
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| Enzyme Assay |
In vitro kinase assays for MRT59 typically involve measuring the inhibition of recombinant CK1δ or CHK1 kinases using radioisotopic or fluorescence-based methods. A typical protocol: recombinant kinase is incubated with varying concentrations of MRT59 (0.01 nM to 100 μM) in kinase assay buffer containing ATP and a peptide substrate. The reaction is incubated for 30-60 minutes at 30°C. Phosphorylated substrate is detected by scintillation proximity assay (SPA) or by time-resolved fluorescence resonance energy transfer (TR-FRET). IC₅₀ values are calculated from inhibition curves. Positive controls include staurosporine or other kinase inhibitors.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A375 Cell Tested Concentrations: 5, 20, 40 µM Incubation Duration: 48 hrs (hours) Experimental Results: Significant reduction in cell number by 5 µM. Apoptosis analysis[1] Cell Types: A375 Cell Tested Concentrations: 1, 5, 10, 20, 40, 80 µM Incubation Duration: 48 hrs (hours) Experimental Results: 5 µM induced massive cell death. Western Blot Analysis [1] Cell Types: A375 Cell Tested Concentrations: 0.2, 1, 5, 10, 20, 40, 80 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of p53, MDM2 and p21 proteins stable and stable E2F-1 unstable, From 0.2 µM to 5 µM. In vitro cell-based assays for MRT59 are performed using cancer cell lines such as HCT116 or MCF-7. A typical protocol: cells are seeded in 96-well plates and treated with MRT59 at concentrations ranging from 0.01 to 100 μM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. p53 pathway activation is assessed by measuring p53 and p21 protein levels by Western blot. E2F-1 protein levels are measured by Western blot. Cell cycle distribution is analyzed by propidium iodide staining. Apoptosis is assessed by Annexin V/PI staining and flow cytometry. Each condition is tested in triplicate. |
| Animal Protocol |
In vivo animal studies for MRT59 are conducted in mouse xenograft models of cancer. A typical protocol: immunocompromised mice are inoculated subcutaneously with cancer cells. When tumors reach 50-100 mm³, mice are randomized to receive MRT59 via oral gavage or intraperitoneal injection at doses of 10-100 mg/kg, daily or every other day, for 2-4 weeks. Tumor volumes are measured with calipers every 2-3 days, and body weight is monitored for toxicity. At study termination, tumors are harvested for histopathological examination and biomarker analysis (e.g., p53, p21, E2F-1 by IHC or Western blot).
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MRT59 have been partially characterized. The compound is soluble in DMSO. Its plasma half-life, volume of distribution, protein binding, and oral bioavailability have been evaluated in preclinical models. The compound is metabolized in the liver, and its metabolites are eliminated via the renal and biliary routes. Specific pharmacokinetic parameters are available from preclinical study reports. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for MRT59 are limited to preclinical studies. The compound has not undergone formal toxicology testing for regulatory purposes. Standard laboratory safety precautions should be followed when handling MRT59: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| References | |
| Additional Infomation |
Additional information for MRT59: The compound has a CAS number of 1401731-54-1. Its molecular formula is C₁₅H₁₄N₄O and molecular weight is 266.30 g/mol. Synonyms include MRT00033659. It is a potent broad-spectrum kinase inhibitor against CK1 (IC₅₀ = 0.9 µM for CK1δ) and CHK1 (IC₅₀ = 0.23 µM). It induces p53 pathway activation and E2F-1 destabilisation. Purity is typically ≥98%. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C15H14N4O
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| Molecular Weight |
266.297862529755
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| Exact Mass |
266.116
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| CAS # |
1401731-54-1
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| PubChem CID |
66555775
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
362
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C)NC1=CC=CC(=C1)C1C=NC2C(=C(C)NN=2)C=1
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| InChi Key |
YFBPGSDPFRCNOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14N4O/c1-9-14-7-12(8-16-15(14)19-18-9)11-4-3-5-13(6-11)17-10(2)20/h3-8H,1-2H3,(H,17,20)(H,16,18,19)
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| Chemical Name |
N-[3-(3-methyl-2H-pyrazolo[3,4-b]pyridin-5-yl)phenyl]acetamide
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| Synonyms |
MRT-59; MRT 59; MRT59
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ~83.33 mg/mL (~312.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (15.66 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 41.7 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: ≥ 4.17 mg/mL (15.66 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 41.7 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: ≥ 4.17 mg/mL (15.66 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 | 3.7552 mL | 18.7758 mL | 37.5516 mL | |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 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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