NL-26
NL-26 is a Topoisomerase I inhibitor. NL-26 stabilizes the covalent Topoisomerase I (Topo I)-DNA complex, prevents DNA religation and triggers the DNA damage response. NL-26 induces G2/M cell cycle arrest and apoptosis in cancer cells. NL-26 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C21H19N3O4
- Molecular Weight:377.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NL-26 (48 h) potently inhibits the proliferation of HCT116 human colon cancer cells in vitro, with a GI50 of 1.03 μM[1].
NL-26 (48 h) inhibits proliferation of A549 human lung cancer cells (GI50 = 4.35 μM) and 4T1 mouse breast cancer cells (GI50 = 4.84 μM) in vitro, with minimal activity against HL-60, PC-3, HepG2, and normal H9C2 cells (GI50 >10 μM)[1].
NL-26 (0.6-2.4 μM; 7-10 days) potently and dose-dependently inhibits long-term colony formation of HCT116 human colon cancer cells in vitro, with near-complete suppression at 2.4 μM[1].
NL-26 (0.6-2.4 μM; 12 h) dose-dependently induces G2/M phase cell cycle arrest in HCT116 human colon cancer cells in vitro, with a 37.4% G2/M population at 2.4 μM after 12 h of treatment[1].
NL-26 (0.6-2.4 μM; 24 h) dose-dependently induces apoptosis in HCT116 human colon cancer cells in vitro, with a total apoptotic rate of 39.3% at 2.4 μM after 24 h of treatment[1].
NL-26 (0.6-2.4 μM; 8 h) dose-dependently activates the DNA damage response in HCT116 human colon cancer cells in vitro, as evidenced by increased γH2AX and PARP-1 protein levels after 8 h of treatment[1].
NL-26 (0.6-2.4 μM; 24 h) dose-dependently inhibits the migratory capacity of HCT116 human colon cancer cells in vitro, reducing wound closure to 20.53% at 2.4 μM after 24 h of treatment[1].
NL-26 (0.6-2.4 μM; 24 h) dose-dependently inhibits the invasive capacity of HCT116 human colon cancer cells in vitro after 24 h of treatment[1].
NL-26 (0.6-2.4 μM; 8 h) dose-dependently modulates apoptotic regulatory proteins in HCT116 human colon cancer cells in vitro, downregulating XIAP and Bcl-2 and upregulating Cleaved Caspase-3 after 8 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:7-10 days
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Result:Suppressed colony formation of HCT116 cells in a dose-dependent manner.
Almost completely eliminated colony growth at the highest concentration (2.4 μM).
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:12 h
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Result:Induced G2/M phase arrest in a dose-dependent manner.
Increased the G2/M phase cell population from 24.3% (control) to 37.4% at 2.4 μM.
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner.
Increased the total apoptotic rate from 9.9% (control) to 39.3% at 2.4 μM.
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:24 h
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Result:Significantly attenuated the wound closure rate of HCT116 cells in a dose-dependent manner.
Restricted the healing rate to 20.53% at the highest concentration (2.4 μM) at 24 h.
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:24 h
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Result:Significantly reduced the number of invasive HCT116 cells in a dose-dependent manner compared to the control group.
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Cell Line:HCT116 human colon cancer cells
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Concentration:0.6, 1.2 and 2.4 μM
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Incubation Time:8 h
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Result:Induced a dose-dependent increase in γH2AX and PARP-1 protein levels, markers of DNA double-strand breaks and DNA damage response activation, respectively.\nInduced a dose-dependent downregulation of anti-apoptotic proteins XIAP and Bcl-2.
Induced a dose-dependent upregulation of pro-apoptotic Cleaved Caspase-3.
| Species | Dose | Route | C0 | Tmax | T1/2 | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | CL | Vd |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | 746.4 ng/mL | 0.03 h | 3.7 h | 1979.7 ng·h/mL | 1986.5 ng·h/mL | 3.641 h | 3.673 h | 2.52 L/h/kg | 10.91 L/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu (female, SPF-grade, subcutaneous HCT116 xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.v.; every other day; 14 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 55.1%.
Markedly downregulated the proliferation marker Ki-67 in tumor tissues.
Showed no signs of systemic toxicity; maintained stable body weight comparable to control group, and showed no treatment-related lesions or tissue damage in major organs upon histopathological analysis.
Chemical Information
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Molecular Weight 377.39
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Formula C21H19N3O4
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SMILES
O=C1COC2=CC=C3C(C=C(OC3=C2N1)C4=CC=C(C=C4)N5CCNCC5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NL-26 Related Classifications
HY-182748 Related Classifications
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- NL-26
- NL26
- NL 26
- Topoisomerase
- DNA/RNA Synthesis
- Apoptosis
- HCT116 human colon cancer cells
- Topo I-DNA covalent complex
- apoptosis
- G2/M phase cell cycle arrest
- Topoisomerase I
- DNA damage response
- 4T1 mouse breast cancer cells
- A549 human lung cancer cells
- HCT116 xenograft mice
- colorectal cancer
- Inhibitor
- inhibitor
- inhibit