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.
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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