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262017 APE1 Inhibitor III - Calbiochem

262017
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₂₁N₃OS₂

Products

Catalogue NumberPackaging Qty/Pack
262017-10MG 10 mg
Description
OverviewA 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 (t1/2 = 80 min).
Catalogue Number262017
Brand Family Calbiochem®
SynonymsN-(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
References
ReferencesRai, G., et al. 2012. J. Med. Chem. 55, 3101.
Product Information
FormBrown solid
Hill FormulaC₁₉H₂₁N₃OS₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetAPE1
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

APE1 Inhibitor III - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

APE1 Inhibitor III - Calbiochem Certificates of Analysis

TitleLot Number
262017

References

Reference overview
Rai, G., et al. 2012. J. Med. Chem. 55, 3101.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision05-April-2017 JSW
SynonymsN-(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
DescriptionA 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 (t1/2 = 80 min).
FormBrown solid
Intert gas (Yes/No) Packaged under inert gas
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (2.5 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesRai, G., et al. 2012. J. Med. Chem. 55, 3101.