2. Immunology/Inflammation
  3. NO Synthase IFNAR
  4. nNOS-IN-2 trihydrochloride

nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways.

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nNOS-IN-2 trihydrochloride

nNOS-IN-2 trihydrochloride Chemical Structure

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nNOS-IN-2 trihydrochloride Related Antibodies

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Description

nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways[1].

IC50 & Target

nNOS

1.7 nM (Ki, human nNOS)

nNOS

2.3 nM (Ki, rat nNOS)

In Vitro

nNOS-IN-2 (compound 9) trihydrochloride induces cytotoxicity in human melanoma A375 and SK-MEL-28 cells, with EC50 values of 2.94 μM and 2.08 μM, respectively, and exhibits lower toxicity toward human primary fibroblasts than the lead compound HH044[1].
nNOS-IN-2 trihydrochloride (5 μM) reduces the basal PD-L1 expression level in human melanoma A375 cells to 70% of that in the control group, and effectively inhibits IFN-γ-induced PD-L1 upregulation at the concentration of 5 μM[1].
nNOS-IN-2 trihydrochloride reduces glutamate-induced NO accumulation in HT22 cells at a concentration of 0.5 μM[1].
nNOS-IN-2 trihydrochloride (200 μM; 17 h) exhibits moderate blood-brain barrier permeability, with an effective permeability of 6.91×10-6 cm/s at a concentration of 200 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

nNOS-IN-2 trihydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: human melanom A375
Concentration: 5 μM
Incubation Time: with 250 μg/mL IFN-γ
Result: Reduced basal PD-L1 expression levels in human melanoma A375 cells to 70% of the control group.
Effectively inhibited IFN-γ-induced PD-L1 upregulation at a concentration of 5 μM.
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-last T1/2 Bioavailability CL C0 Vss
Mice[1] 3 mg/kg i.v. 0.08 h 87.68 ng/mL 500.82 11.27 h / 85.37 mL/min/kg 2477.24 ng/mL 49.55 L/kg
Mice[1] 10 mg/kg p.o. 0.50 h 14.46 ng/mL 128.81 20.16 h 8 % 2.61 mL/min/kg / /
Molecular Weight

533.92

Formula

C27H31Cl3N4O
SMILES

N=C(C1=CC=CO1)NC2=CC=CC(CNCCC3=CC=C(C4=CC=CC=C4)C=C3CN)=C2.Cl.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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nNOS-IN-2 trihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

nNOS-IN-2 trihydrochlorideNO SynthaseIFNARNitric oxide synthasesNOSInterferon-α/β receptorInterferon-alpha/beta receptorhuman melanoma A375 cellsmelanomaneuronal nitric oxide synthasePD-L1humanhuman melanoma cellsinterferon-gammaSK-MEL-28 cellsratblood-brain barrierInhibitorinhibitorinhibit

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nNOS-IN-2 trihydrochloride
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