| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
MRN complex (MRE11-RAD50-NBS1). Mirin is an inhibitor of the MRN complex, which is a critical sensor of DNA double-strand breaks and an activator of ATM kinase.
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| ln Vitro |
With an IC50 of 66 μM, mirin inhibits the phosphorylation of H2AX. Additionally, mirin prevents the MRN-dependent autophosphorylation of ATM at Ser1981 in response to DSBs as well as the ATM-dependent phosphorylation of the downstream targets Nbs1 and Chk2. Significant G2 arrest is induced by mirin at 50 μM and 100 μM doses. In TOSA4 cells, mirin (10–100 μM) suppresses homology-dependent DNA repair[1]. The Mre11 inhibitor Mirin also caused hypersensitivity in BRCA2-deficient cells[2].
Mirin is an inhibitor of the MRN complex with an IC50 of 12 μM for inhibiting MRN-dependent ATM activation. It inhibits Mre11-associated exonuclease activity. By inhibiting the MRN complex, mirin disrupts DNA double-strand break repair and eliminates the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin sensitizes cells to DNA-damaging agents and has been shown to promote damage by forming double-stranded DNA breaks. |
| ln Vivo |
In vivo, mirin has been used to sensitize viruses to antiviral polyamides (AVP). As an inhibitor of the MRN complex, it disrupts DNA repair and may enhance the efficacy of DNA-damaging therapies.
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| Enzyme Assay |
In vitro enzyme assays for mirin are performed to evaluate its inhibitory activity against the MRN complex. The MRN complex is incubated with DNA substrates and ATP in the presence of varying concentrations of mirin. The inhibition of MRN-dependent ATM activation is measured by assessing ATM phosphorylation, and IC50 values are calculated from the concentration-response curves. Mre11-associated exonuclease activity is measured using fluorescent or radiolabeled DNA substrates.
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| Cell Assay |
In vitro cell-based assays are conducted to evaluate the effects of mirin on DNA repair and cell cycle regulation. Cells are treated with mirin, and DNA damage responses are assessed by measuring ATM phosphorylation, γ-H2AX foci formation, and cell cycle progression. The compound's ability to sensitize cells to DNA-damaging agents is evaluated by measuring cell viability and clonogenic survival following irradiation or treatment with chemotherapeutic agents.
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| Animal Protocol |
In vivo animal studies with mirin are conducted to evaluate its effects on DNA repair and its potential as a sensitizer for cancer therapy. The compound is typically administered via intraperitoneal injection. Its effects on tumor growth, DNA damage responses, and survival are assessed in combination with radiation or chemotherapeutic agents.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for mirin. As a small molecule inhibitor, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for mirin. As an inhibitor of the MRN complex, its toxicity profile would be expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
Mirin is a small molecule inhibitor of the MRN complex that inhibits MRN-dependent ATM activation (IC50 = 12 μM) and Mre11-associated exonuclease activity. It disrupts DNA double-strand break repair and eliminates the G2/M checkpoint. Mirin is used as a research tool to study DNA damage responses and has been investigated as a sensitizer for cancer therapy. The compound is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C10H8N2O2S
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|---|---|
| Molecular Weight |
220.25
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| Exact Mass |
220.03
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| CAS # |
299953-00-7
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| Related CAS # |
(Z)-Mirin;1198097-97-0
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| PubChem CID |
1206243
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| Appearance |
Brown to orange solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
441.6±55.0 °C at 760 mmHg
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| Flash Point |
220.8±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.718
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| LogP |
1.36
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
330
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1/C=C/2\C(=O)N=C(S2)N)O
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| InChi Key |
YBHQCJILTOVLHD-VMPITWQZSA-N
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| InChi Code |
InChI=1S/C10H8N2O2S/c11-10-12-9(14)8(15-10)5-6-1-3-7(13)4-2-6/h1-5,13H,(H2,11,12,14)/b8-5+
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| Chemical Name |
(5E)-2-amino-5-[(4-hydroxyphenyl)methylidene]-1,3-thiazol-4-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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (378.34 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5403 mL | 22.7015 mL | 45.4030 mL | |
| 5 mM | 0.9081 mL | 4.5403 mL | 9.0806 mL | |
| 10 mM | 0.4540 mL | 2.2701 mL | 4.5403 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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