Urease-IN-23
Urease-IN-23 is a cryptococcal urease inhibitor with antifungal activity. AF55 exhibits mixed-type inhibition against cryptococcal urease, binds to both the nickel ion site at the enzyme's catalytic center and the allosteric site, impairs urease catalytic efficiency, simultaneously disrupts fungal virulence structures and damages cell membrane integrity. The IC50 and Ki values of Urease-IN-23 against cryptococcal urease are 54.92 nM and 149.1 nM, respectively. Urease-IN-23 significantly reduces the capsule thickness of Cryptococcus neoformans and Cryptococcus gattii, increases fungal cell membrane permeability, and completely blocks melanin synthesis. Urease-IN-23 shows no toxicity in the Galleria mellonella larval model. Urease-IN-23 can be used in studies related to fungal infections.
For research use only. We do not sell to patients.
- CAS No.: 2180967-88-6
- Formula: C14H16N2O2Se
- Molecular Weight:323.25
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Urease-IN-23 (1.5-24 μM; 48 h) inhibits planktonic growth and urease activity of Cryptococcus neoformans and Cryptococcus gattii clinical isolates and reference strains, with IC50 values ranging from 1.5-24 μM, IC90 values ranging from 1.5-24 μM, ICURE values ranging from 1.5-6 μM, and MFC values ranging from 1.5-24 μM[1].
Urease-IN-23 (12-50 μM; 48-72 h) inhibits biofilm formation and growth of dispersed cells from mature biofilms of Cryptococcus neoformans H99 and Cryptococcus gattii R265, with IC90 values of 12 μM (biofilm formation) and 25-50 μM (dispersed cells), but does not inhibit sessile cells from preformed biofilms[1].
Urease-IN-23 (12 μM; 48 h) significantly reduces capsule thickness in Cryptococcus neoformans H99 and Cryptococcus gattii R265[1].
Urease-IN-23 (6-12 μM; 96 h) completely inhibits melanin production in Cryptococcus neoformans H99 and Cryptococcus gattii R265 after 96 h of incubation[1].
Urease-IN-23 (2×IC90; up to 72 h) rapidly kills Cryptococcus neoformans H99 and Cryptococcus gattii R265 within 2 h of exposure, reducing viability to undetectable levels[1].
Urease-IN-23 (IC90, MFC, 4×MFC; 2 h) significantly increases plasma membrane permeability in Cryptococcus neoformans H99 and Cryptococcus gattii R265 after 2 h of exposure[1].
Urease-IN-23 potently inhibits Cryptococcus neoformans urease in a cell-free assay with a IC50 of 54.92 nM, acting as a mixed-type inhibitor with a Ki of 149.1 nM[1].
Urease-IN-23 acts as a mixed-type inhibitor of Cryptococcus neoformans urease by simultaneously interacting with both the catalytic nickel center and the allosteric site via ionic interactions with Asp626, inducing dynamic conformational changes in the enzyme[1].
Urease-IN-23 (72 h) exhibits cytotoxicity against metastatic breast cancer MCF-7 cells with a CC50 of 75.4 μM after 72 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:larvae (2.0-2.5 cm length, 150-200 mg body mass)[1]
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Dosage:100 mg/kg
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Administration:injected into last left pro-leg; single dose
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Result:Achieved 100% larval survival over 5 days.
Showed high health index scores comparable to control groups.
Chemical Information
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CAS No. 2180967-88-6
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Molecular Weight 323.25
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Formula C14H16N2O2Se
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SMILES
CCOC(C1=C(C)NC(NC1C2=CC=CC=C2)=[Se])=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)