β-Lactamase/Ferroptosis-IN-1
β-Lactamase/Ferroptosis-IN-1 is a dual inhibitor of β-Lactamase and ferroptosis, β-Lactamase/Ferroptosis-IN-1 inhibits NDM-1 (metallo-β-lactamase, MBLs, IC50 = 1.8 μM) and KPC-2 (serine-β-lactamase, SBLs, IC50 = 2.6 μM). β-Lactamase/Ferroptosis-IN-1 exerts synergistic antibacterial effects with antibiotics against multidrug-resistant Gram-negative bacteria (MDR-GNB), and alleviates LPS (HY-D1056)-induced acute lung injury by inhibiting ferroptosis via upregulating FTH1 and GPX4 expression and reducing MDA levels. β-Lactamase/Ferroptosis-IN-1 can be used for the study of MDR-GNB infections and acute lung injury.
For research use only. We do not sell to patients.
- CAS No.: 3115648-56-8
- Formula: C13H10BNO3Se
- Molecular Weight:317.99
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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
All Beta-lactamase Isoforms
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Biological Activity
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NDM-1 1.8 μM (IC50) |
KPC-2 2.6 μM (IC50) |
GPX4 |
β-Lactamase/Ferroptosis-IN-1 (compound E3f) (128 μg/mL; 20 h) (IC50 = 1.8 μM against NDM-1 and IC50 = 2.6 μM against KPC-2) in combination with β-lactam antibiotics restores antibiotic susceptibility in clinically isolated resistant strains producing single enzymes (NDM-1 or KPC-2) or dual enzymes (NDM-1 and KPC-2), and effectively restores the antibacterial activity of β-lactams against strains producing serine β-lactamases (TEM-1, CTX-M-14, and BlaEC), including A. baumannii 10-12, A. baumannii 9-1, and E. coli 8-118[1].
β-Lactamase/Ferroptosis-IN-1 (10 μM; preincubation for 2 h) reverses the LPS-induced upregulation of IL-1β, IL-6 and TNF-α expression compared with the control in BV-2 cells[1].
β-Lactamase/Ferroptosis-IN-1 (0.18-18 μM; 10 min) effectively irreversibly inhibits NDM-1, with residual enzyme activity recovering from only 9% to 61%[1].
β-Lactamase/Ferroptosis-IN-1 (1 mM; 20 h) reduces the zinc ion content of NDM-1 by approximately 34%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 cells
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Concentration:10 mM
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Incubation Time:preincubation for 2 h
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Result:Suppressed the expression of IL-1β, IL-6, and TNF-α) in LPS-activated BV-2 microglia.
β-Lactamase/Ferroptosis-IN-1 (100-300 mg/kg; i.p.; single dose; for 14 days) exhibits a favorable safety profile in C57BL/6 mice[1].
β-Lactamase/Ferroptosis-IN-1 (40 mg/kg; i.g.; first administration at 6 h post-infection, re-dose at 24-48 h) in combination with Meropenem (HY-13678) significantly reduces bacterial loads in the liver and spleen, as well as serum levels of TNF-α, IL-1β, and IL-6, β-Lactamase/Ferroptosis-IN-1 monotherapy exhibits no bactericidal effect in a murine intra-abdominal infection model induced by E. coli ATCC BAA 2452 in male Kunming mice (6-week-old)[1].
β-Lactamase/Ferroptosis-IN-1 (20 mg/kg; i.p.; single dose at 1 h prior to LPS challenge) upregulates the ferroptosis-related proteins FTH1 and GPX4, and reduces MDA levels in LPS-induced acute lung injury (ALI) model in male Kunming mice (6-week-old)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine intra-abdominal infection model induced by E. coli ATCC BAA 2452 in male Kunming mice (6-week-old)[1].
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Dosage:40 mg/kg
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Administration:i.g.; first administration at 6 h post-infection, re-dose at 24-48 h
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Result:Combined with Meropenem reduced bacterial loads in the liver and spleen compared with Meropenem.
Showed lower serum levels of TNF-α, IL- 1β and IL-6.
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Animal Model:LPS-induced acute lung injury (ALI) model in male Kunming mice (6-week-old)[1].
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Dosage:20 mg/kg
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Administration:i.p.; single dose at 1 h prior to LPS challenge
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Result:Alleviated the pathological damage induced by LPS.
Upregulated FTH1 expression level.
Reversed the substantial reduction of GPX4 levels in lung tissues induced by LPS.
Suppressed the LPS-triggered elevation of MDA in mouse lung tissues.
Chemical Information
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CAS No. 3115648-56-8
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Molecular Weight 317.99
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Formula C13H10BNO3Se
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SMILES
O=C1N(C2=CC(B(O)O)=CC=C2)[Se]C3=CC=CC=C13
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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)
β-Lactamase/Ferroptosis-IN-1 Related Classifications
HY-184667 Related Classifications
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