PUN-96956
PUN-96956 is an inhibitor of the β-barrel assembly machine (BAM) complex. By inhibiting the folding of β-barrel outer membrane proteins (OMPs) and their insertion into the outer membrane, PUN-96956 disrupts outer membrane integrity and induces the cell envelope stress response. PUN-96956 can be used in studies of bacterial infections caused by ESKAPE pathogens, uropathogenic Escherichia coli, and Gram-positive bacteria.
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- CAS. Nr.: 1144496-95-6
- Formel: C21H33ClN2
- Molecular Weight:348.96
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | LD50 |
20 μM
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Cytotoxicity against HEK293 human embryonic kidney cells, measured via Cell Titer Glo luminescence assay after 48 h incubation at 37°C with 5% CO2.
Cytotoxicity against HEK293 human embryonic kidney cells, measured via Cell Titer Glo luminescence assay after 48 h incubation at 37°C with 5% CO2.
|
34125508 |
In Vitro
PUN-96956 (compound 2) (12-100 μM; 10 h) inhibits the growth of *Escherichia coli* MC4100 wild-type cells and cells expressing FhuA ΔC/4L in a dose-dependent manner[1].
PUN-96956 (12-200 μM; 10 h) inhibits the growth of various Gram-negative bacteria in a dose-dependent manner[1].
PUN-96956 (3 h) activates the σE cell envelope stress response in Escherichia coli TOP10F′ cells with an EC50 of 6 μM, and does not induce intracellular heat shock stress[1].
PUN-96956 (up to 200 μM; 10 h) exhibits enhanced growth inhibitory activity in Escherichia coli MC4100 ΔsurA, ΔbamB, and ΔdegP cells[1].
PUN-96956 (12 μM; 3 h) reduces the steady-state levels of the β-barrel outer membrane proteins OmpF, OmpC, OmpA, and BamA in Escherichia coli TOP10F′ cells without affecting lipoprotein levels[1].
PUN-96956 (12-25 μM; 2.5 h) reduces the de novo biogenesis of the β-barrel outer membrane protein PhoE in Escherichia coli TOP10F′ cells by interfering with membrane targeting or insertion (rather than folding) processes[1].
PUN-96956 (12 μM; 2.5 h) impairs the secretion of the autotransporter protein Hbp in Escherichia coli MC1061 degP::S210A cells by inhibiting the assembly of the C-terminal β-barrel domain of Hbp, and simultaneously upregulates σE stress-regulated DegP[1].
PUN-96956 (25-100 μM; 5 min preincubation, up to 80 min folding reaction) inhibits the BAM-dependent folding and insertion of the β-barrel protein OmpT in vitro, with an EC50 of 58.3 μM. It exerts its effect primarily during the folding process rather than by directly inhibiting the protease activity of OmpT[1].
PUN-96956 (up to 60 μM; 48 h) exhibits cytotoxicity against HEK293 human embryonic kidney cells, with an LD50 of 20 μM[1].
PUN-96956 (0.08-60 μM; 3 h) induces dose-dependent σE and RprA stress responses in Escherichia coli TOP10F' cells without affecting the GroES stress response; after 3 h of incubation, a maximum 2.5-fold induction of σE and 5-fold induction of RprA are achieved at a concentration of 60 μM[1].
PUN-96956 (100 μM) disrupts the assembly of OmpT via the BAM complex in proteoliposomes in a dose-dependent manner, with the inhibitory effect reaching a peak at 100 μM, and does not inhibit the protease activity of fully folded OmpT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Escherichia coli TOP10F′ cells
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Concentration:12 μM
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Incubation Time:3 h
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Result:Reduced steady-state levels of major β-barrel OMPs (OmpF, OmpC, OmpA) and BamA, while levels of BamB and LpoB (lipoproteins) remained largely unaffected.
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Cell Line:Escherichia coli TOP10F′ cells expressing PhoE
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Concentration:12, 25 μM
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Incubation Time:3 h
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Result:Reduced total levels of PhoE in a dose-dependent manner.
PhoE remained heat-modifiable regardless of compound treatment, indicating interference with membrane targeting/insertion rather than folding.
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Cell Line:Escherichia coli MC1061 degP::S210A cells
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Concentration:12 μM
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Incubation Time:3 h
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Result:Caused accumulation of pro-Hbp in cell lysates, reduced levels of cleaved Hbp β-barrel domain, and decreased secretion of mature Hbp passenger into the spent medium.
Also upregulated σE stress-regulated DegP.
Chemical Information
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CAS. Nr. 1144496-95-6
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Molecular Weight 348.96
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Formel C21H33ClN2
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SMILES
ClC1=CC=C(C=C1)CC2(CCNC3CCN(C)CC3)CCCCC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- PUN-96956
- 1144496-95-6
- PUN96956
- PUN 96956
- Bacterial
- β-barrel assembly machine complex
- β-barrel outer membrane protein
- Escherichia coli
- Gram-positive bacterial species
- HEK293 human embryonic kidney cells
- Rcs cell envelope stress response
- σE cell envelope stress response
- uropathogenic escherichia coli
- Gram-negative bacterial species
- ESKAPE pathogens
- Inhibitor
- inhibitor
- inhibit