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APE1 Inhibitor III

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

• 別名: 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
• 実験式（ヒル表記法）: C₁₉H₂₁N₃OS₂
• CAS番号: 524708-03-0
• 分子量: 371.52
• MDL番号: MFCD11984329
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: brown
• 溶解性: DMSO: 2.5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: CC(C)N(CC1)CC2=C1C(C3=NC4=C(C=CC=C4)S3)=C(S2)NC(C)=O

詳細

詳細

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).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
APE1

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable