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Mirin ATM/ATR inhibitor

Name: Mirin
SKU: S8096
Availability: InStock
Rating: 5 (34 reviews)

Cat.No.S8096

Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. This compound inhibits MRN-dependent activation of ATM.

Chemical Structure

Molecular Weight: 220.25

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.79%

99.79

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Chemical Information, Storage & Stability

Molecular Weight	220.25	Formula	C₁₀H₈N₂O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1198097-97-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	OC1=CC=C(C=C1)\C=C2/SC(=N)NC2=O

Solubility

In vitro
Batch:

DMSO : 44 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (4.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 ddH₂O, 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.

Mechanism of Action

Targets/IC₅₀/Ki	MRN ^[1] ATM ^[1]
In vitro	Mirin inhibits DSB-induced ATM activation, the ATM-dependent phosphorylation of the downstream targets Nbs1 and Chk2 and the MRN-dependent autophosphorylation of ATM at Ser1981 in response to DSBs. This compound also inhibits the G2 checkpoint in TOSA4 cells, and homology-dependent DNA repair in HEK293 cells. ^[1] In cells with integrated HPV16 (SiHa), it sensitizes HPV episomes to PA25 resulting in a ∼5-fold reduction of the PA25 IC50. ^[2] Pretreatment with this chemical also decreases cell viability and inhibits proliferating cell nuclear antigen expression in cisplatin-treated human embryonic kidney 293 cells. ^[3]
Kinase Assay	Nuclease assay
Kinase Assay	Reactions with oligonucleotide nonhairpin substrates contains 25 mM MOPS (pH 7.0), 60 mM KCl, 0.2% Tween 20, 2 mM DTT, 1 mM or 5 MnCl₂ (or 5 mM MgCl₂, or 5 mM CaCl₂), 0.1 pmol of DNA substrate, and 0.3 pmol of Mre11 (or an equivalent amount of Mre11 complexed with Rad50) in a volume of 10 μl, and are incubated at 37°C for 30 min. SDS, EDTA, and proteinase K are then added to final concentrations of 0.2%, 5 mM, and 0.1 mg/ml, respectively, and incubated for another 15 min. 4 μl of each reaction is mixed with 4 μl of formamide loading buffer, and then loaded onto a sequencing gel containing 10% acrylamide and 7 M urea. After the run, each gel is analyzed using a phosphorimaging system. Reactions containing hairpin substrates are identical to those with nonhairpin substrates except that 3 pmol of this compound is added to reactions as indicated, and the reactions are incubated at room temperature overnight. Nonhomologous end-joining reactions contains 25 mM MOPS (pH 7.0), 60 mM KCl, 0.2% Tween 20, 2 mM DTT, 4 mM MgCl₂, 2 mM MnCl₂, 0.5 mM ATP, 4 ng of plasmid DNA, 10% polyethylene glycol, 0.01 pmol of human DNA ligase I, and 0.06 pmol of this chemical or 0.1 units of E. coli exonuclease III (GIBCO-BRL), in a volume of 10 μl. After incubation at 37°C for 25 min, Tween 20 is added to a final concentration of 0.5%, and a 2.5 μl aliquot is amplified by PCR using primers DAR5 and DAR147. PCR products are cloned using the TA cloning kit and sequenced using an automated ABI Capillary Genetic Analyzer.
In vivo	Mirin in nanoparticles resulted in a sharp impairment of tumor growth, associated with DDR activation, p53 accumulation, and cell death.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18176557/ [2] https://pubmed.ncbi.nlm.nih.gov/24098381/ [3] https://pubmed.ncbi.nlm.nih.gov/26056972/ [4] https://pubmed.ncbi.nlm.nih.gov/30166519/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		18176557

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