TH5487

Catalog No.S8913 Batch:S891301

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Technical Data

Formula

C19H18BrIN4O2
Molecular Weight 541.18 CAS No. 2304947-71-3
Solubility (25°C)* In vitro DMSO 10 mg/mL (18.47 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.
Targets
OGG1 [1]
(Cell-free assay)
342 nM
In vitro

TH5487 increases the melting temperature of OGG1 in human cells.TH5487 impaires repair of genomic 8-oxoG induced by KBrO3.TH5487 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. TH5487 is efficacious in vivo, suggesting that the compound could be used for the treatment of inflammatory conditions. [1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HEK 293T cells Wild-type, HEK 293T cells OGG1-KO, MLE12, hSAECs

  • Concentrations

    5 μM

  • Incubation Time

    1 h

  • Method

    --
Animal Study:

[1]
  • Animal Models

    mice (50% female and 50% male) of which lungs are TNFα-challenged intranasally (20 ng/ml)

  • Dosages

    30 mg/kg

  • Administration

    IP

Selleck's TH5487 has been cited by 3 publications

Inhibition of OGG1 ameliorates pulmonary fibrosis via preventing M2 macrophage polarization and activating PINK1-mediated mitophagy [ Mol Med, 2024, 30(1):72] PubMed: 38822247
RELA∙8-Oxoguanine DNA Glycosylase1 Is an Epigenetic Regulatory Complex Coordinating the Hexosamine Biosynthetic Pathway in RSV Infection [ Cells, 2022, 11(14)2210] PubMed: 35883652
8-oxoguanine DNA glycosylase1 recognizes oxidatively-generated epitranscriptomic marks on nascent mRNAs to promote RSV replication [ Research Square, 2021, 10.21203/rs.3.rs-515369/v1] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.