MALT1-IN-16
MALT1-IN-16 is an orally active MALT1 inhibitor with an IC50 of 11 nM against hMALT1. MALT1-IN-16 inhibits NF-κB signaling. MALT1-IN-16 inhibits IL-2 production and germinal center formation. MALT1-IN-16 can be used for research on Sjögren's syndrome.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C19H21ClN8O
- Peso molecular:412.88
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IL-22 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
174 nM
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Inhibition of NF-κB signaling in human Jurkat cells.
Inhibition of NF-κB signaling in human Jurkat cells.
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5437771 |
In Vitro
MALT1-IN-16 (0.5 h) exhibits moderate metabolic stability in mouse liver microsomes, with 56% remaining after 0.5 h[1].
MALT1-IN-16 (10 μM) exhibits weak direct inhibition of CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4, with the highest values observed for CYP2C9 (37%) and CYP3A4 (31%)[1].
MALT1-IN-16 has a hERG IC50 greater than 30 μM[1].
MALT1-IN-16 binds to mouse plasma proteins at a rate of 83.6%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, n=5)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:single administration
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Result:Produced dose-dependent suppression of plasma IL-2 at both 4 h and 8 h after dosing, with greater suppression at 30 mg/kg than at 10 mg/kg.
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Animal Model:BALB/cAnNCrlCrlj (male, 8 weeks, n=5)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; twice daily (bid); Days 0-8
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Result:Suppressed splenic germinal center formation at both 30 mg/kg bid and 60 mg/kg bid; maximum suppression was observed at 30 mg/kg bid.
Produced dose-dependent reduction of peripheral blood Tregs at 30 and 60 mg/kg bid.
Chemical Information
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Peso molecular 412.88
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Fòrmula C19H21ClN8O
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SMILES
O=C([C@H]1[C@H](C)CN(C2=NC=CC=C2N)CC1)NC3=CC(Cl)=C(N4N=CC=N4)N=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MALT1-IN-16 Related Classifications
HY-190736 Related Classifications
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