262017

APE1 Inhibitor III

The APE1 Inhibitor III controls the biological activity of APE1. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Sinónimos: APE1 Inhibitor III, Apurinic Endonuclease 1 Inhibitor III, Apurinic/Apyrimidinic Endonuclease 1 Inhibitor III, N-(3-(1,3-Benzo[d]thiazol-2-yl)-6-isopropyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl)acetamide, N-(3-(1,3-Benzo[d]thiazol-2-yl)-6-isopropyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl)acetamide, Apurinic Endonuclease 1 Inhibitor III, Apurinic/Apyrimidinic Endonuclease 1 Inhibitor III
• Fórmula empírica (notación de Hill): C₁₉H₂₁N₃OS₂
• Número de CAS: 524708-03-0
• Peso molecular: 371.52
• MDL number: MFCD11984329
• UNSPSC Code: 12352200
• NACRES: NA.28

Propiedades

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: brown
• solubility: DMSO: 2.5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: CC(C)N(CC1)CC2=C1C(C3=NC4=C(C=CC=C4)S3)=C(S2)NC(C)=O

Descripción

General description

A cell-permeable benzothiazolyltetrahydrothienopyridine compound that acts as a potent, competitive, and active site targeting inhibitor of APE1 (IC₅₀ = 2.0 µM in a fluorescence based HTS assay; and 12 .0 µM in a radiotracer incision assay). Shown to block APE1 activity in HEK293T and HeLa cells extract (IC₅₀ = 600 nM) and increase genomic AP site accumulation. Potentiates the cytotoxicity of DNA-damaging alkylating agents in HeLa cells by ~3-fold. Exhibits favorable pharmacokinetic properties and desirable ADME attributes. Due to its lipophilic nature, it crosses the blood-brain barrier rather easily and shows desirable stability (t_1/2 = 80 min).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
APE1

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Rai, G., et al. 2012. J. Med. Chem.55, 3101.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable