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TH5487 OGG1 inhibitor

Name: TH5487
Brand: Selleck Chemicals
SKU: S8913
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8913

TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.

Chemical Structure

Molecular Weight: 541.18

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

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	DNA/RNA Synthesis HDAC Topoisomerase PPAR PARP Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DHFR Nucleoside Analog/Antimetabolite DNA alkylator Telomerase Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR Alkylating Agent NUDIX High-mobility Group MTH1 G-quadruplex SMN FENs WRN Pax
Related Products	SU0268 OGG1-IN-08 TH10785

Chemical Information, Storage & Stability

Molecular Weight	541.18	Formula	C₁₉H₁₈BrIN₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2304947-71-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCC1N2C3=C(C(=CC=C3)Br)NC2=O)C(=O)NC4=CC=C(C=C4)I

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (18.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 60 mg/mL (110.86 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

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 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (2.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 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.

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	OGG1 ^[1] (Cell-free assay) 342 nM
In vitro	TH5487 increases the melting temperature of OGG1 in human cells. This compound impaires repair of genomic 8-oxoG induced by KBrO₃. It preventes OGG1 binding to its genomic substrate in living cells.^[1]
In vivo	To assess whether TH5487 could down-regulate chemotactic (C-C and C-X-C) mediators in vivo, we challenge mouse lungs with TNFα and profile the gene expression of proinflammatory mediators. This compound is efficacious in vivo, suggesting that it could be used for the treatment of inflammatory conditions. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/30442810/

Tech Support

Handling Instructions

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