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APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.
Pack Size | Price | Availability | Quantity |
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1 mg | $62 | In Stock |
Description | APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells. |
Targets&IC50 | qHTS assay:2 μM, Radiotracer incision assay:12 μM |
In vitro | In the qHTS assay, APE1-IN-1 (compound 3) displays an IC50 of 2 μM, while in a radiotracer incision assay (RIA), it exhibits an IC50 of 12 μM[1]. In a dose-dependent manner, APE1-IN-1 (at concentrations of 0, 1, 3, 10, 30, or 100 μM for 15 minutes) inhibits AP site incision in HeLa whole cell extracts[1]. Furthermore, APE1-IN-1 (at concentrations ranging from 5 to 30 μM for 24 hours) demonstrates cytotoxic activity against HeLa cells and enhances the activity of methyl methansulfonate and Temozolomide[1]. |
In vivo | Administered at a single dosage of 30 mpk via intraperitoneal injection, APE1-IN-1 demonstrates favorable pharmacokinetic properties[1]. |
Molecular Weight | 371.52 |
Formula | C19H21N3OS2 |
Cas No. | 524708-03-0 |
Smiles | CC(C)N1CCc2c(C1)sc(NC(C)=O)c2-c1nc2ccccc2s1 |
Storage | store at low temperature | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 10 mg/mL (26.92 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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