2. Apoptosis
  3. Apoptosis MDM-2/p53
  4. APE1-IN-2

APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals.

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APE1-IN-2 Chemical Structure

APE1-IN-2 Chemical Structure

CAS No. : 2923433-95-6

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APE1-IN-2 Related Antibodies

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Description

APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals[1].

In Vitro

APE1-IN-2 (compound AP1) can strongly inhibit the growth of malignant cells, including Cisplatin-resistant cancer cells, with up to 18.11 times inhibition compared with Cisplatin (HY-17394)[1].
APE1-IN-2 (500 nM, 24 h) arrests the cell cycle in A549 and MCF7 cells[1].
APE1-IN-2 (10 μM, 24 h) induces p53-dependent apoptosis in A549 cells[1].
APE1-IN-2 (0-250 μM, 72 h) inhibits AP-cutting activity with an IC50 of 45.14 ± 17.37 μM[1].
APE1-IN-2 can directly inhibit the AP endonuclease activity of APE1, leading to an interruption of miRNA processing and upregulation of the tumor suppressor PTEN[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

APE1-IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549 (non-small cell lung cancer), MCF7 (breast cancer), U251 (glioblastoma), A375 (melanoma), PC3 (prostate cancer), and HEP-G2 (hepatocarcinoma) cell lines
Concentration:
Incubation Time: 72 h
Result: Demonstrated more potent antiproliferation effects than Cisplatin (HY-17394), with IC50 of 0.45 ± 0.03, 0.43 ± 0.03, 4.70 ± 0.14, 0.39 ± 0.03, 5.65 ± 0.21, and 3.53 ± 0.31 μM in A549, MCF7, U251, A375, PC3, and HEP-G2 cell lines, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 and MCF7 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Induced the most severe S-phase arrest in A549 and MCF7 cells.

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Caused apoptosis in approximately 38.7% (22.9% early apoptosis and 15.8% late apoptosis) of cancer cells.

Western Blot Analysis[1]

Cell Line: A549 and HEK-293T cell lines
Concentration: 0, 16, 40, 100, 250 μM
Incubation Time: 72 h
Result: Significantly increased the level of p53 by 2.09 ± 0.51-fold. Slightly raised the levels of p53, γH2A.X, and cl.PARP in HEK-293T. Inhibited AP-cutting activity with an IC50 value of 45.14 ± 17.37 μM.
In Vivo

APE1-IN-2 (compound AP1) (2 mg/kg, IP, once every 3 days for 15 days) exhibits an antitumor effect on the A549 xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (5 week-old, female, 16 ± 2 g of body weight bearing A549 xenograft tumors)[1]
Dosage: 2 mg/kg
Administration: IP, once every 3 days for 15 days
Result: Exhibited a 3.86-fold xenograft tumor inhibitory activity compared to Cisplatin. Did not significantly alter the body weight of mice, improving its sufficient safety.
Molecular Weight

522.21

Formula

C9H12Cl2N4O5Pt
CAS No.
Unlabeled CAS

SMILES

O[Pt](Cl)(Cl)(OC(C1=CC2=CC=CC([N+]([O-])=O)=C2N1)=O)([NH3])[NH3]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APE1-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APE1-IN-22923433-95-6ApoptosisMDM-2/p53pri-miR-221pri-miR-222A549MCF7U251A375PC3HEP-G2anticancerCisplatin-resistantDNA damageInhibitorinhibitorinhibit

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