GlmU-IN-1
GlmU-IN-1 is an inhibitor of the GlmU acetyltransferase domain in Escherichia coli and Haemophilus influenzae. GlmU-IN-1 acts as a competitive inhibitor of AcCoA and a non-competitive inhibitor of GlcN-1-P. GlmU-IN-1 targets the acetyltransferase domain of bacterial GlmU, interferes with the biosynthesis of UDP‑GlcNAc, and impairs bacterial cell wall integrity. GlmU-IN-1 can be used for the research of Gram-negative bacterial infections.
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- CAS No.: 104926-84-3
- Formule: C9H7Cl2N3O
- Masse moléculaire:244.08
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
>150 μg/mL
|
Cytotoxicity against human liver carcinoma HepG2 cells assessed via MTT assay after 24 h incubation.
Cytotoxicity against human liver carcinoma HepG2 cells assessed via MTT assay after 24 h incubation.
|
26563552 |
In Vitro
GlmU-IN-1 (5175178) (0.39-100 μM; 30 min) potently and specifically inhibits the acetyltransferase activity of purified E. coli GlmU with an IC50 of 1.40 μM, and inhibits the acetyltransferase activity of purified H. influenzae GlmU with an IC50 of 79.92 μM. It acts as a competitive inhibitor against AcCoA and a non-competitive inhibitor against GlcN-1-P[1].
GlmU-IN-1 (4 μg/mL; 30 min) disrupts the cell membrane permeability of E. coli ATCC 25922[1].
GlmU-IN-1 (24 h) shows no cytotoxicity against HepG2 cells, with its CC50 >150 μg/mL[1].
GlmU-IN-1 (0.0625-32 μg/mL; 24 h) exhibits bactericidal activity against E. coli ATCC 25922 (MIC 4 μg/mL, MBC 32 μg/mL), and also shows antibacterial activity against NDM1-producing A. baumanii and K. pneumoniae isolates[1].
GlmU-IN-1 inhibits the growth of E. coli BL21 (DE3) by targeting GlmU. Compared with wild-type and empty vector control cells, the bacterial IC50 of GlmU-overexpressing cells is four times higher[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 104926-84-3
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Masse moléculaire 244.08
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Formule C9H7Cl2N3O
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SMILES
OC1=C2N=C(C=CC2=C(C=C1Cl)Cl)NN
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)