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262017

Sigma-Aldrich

APE1 Inhibitor III

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C19H21N3OS2
CAS Number:
524708-03-0
Molecular Weight:
371.52
MDL number:
MFCD11984329
UNSPSC Code:
12352200
NACRES:
NA.28

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

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 (t1/2 = 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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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J-L Yang et al.
Neuropathology and applied neurobiology, 46(4), 375-390 (2019-10-20)
Accumulating studies have suggested that base excision repair (BER) is the major repair pathway of oxidative DNA damage in neurons, and neurons are deficient in other DNA repair pathways, including nucleotide excision repair and homologous recombination repair. However, some studies
Huimin Zhang et al.
Nature communications, 13(1), 4240-4240 (2022-07-23)
Anticancer drugs, such as camptothecin (CPT), trap topoisomerase I (TOP1) on DNA and form TOP1 cleavage complexes (TOP1cc). Alternative repair pathways have been suggested in the repair of TOP1cc. However, how these pathways work with TDP1, a key repair enzyme
Mrinal Srivastava et al.
EMBO reports, 21(6), e49123-e49123 (2020-04-21)
Replication across oxidative DNA lesions can give rise to mutations that pose a threat to genome integrity. How such lesions, which escape base excision repair, get removed without error during replication remains unknown. Our PCNA-based screen to uncover changes in

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