K811
K811 is an orally active ASK1 inhibitor with an IC50 of 6 nM. K811 inhibits glial cell activation in the lumbar spinal cord of SOD1G93A transgenic mice. K811 extends the survival of SOD1G93A transgenic mice, a mouse model of amyotrophic lateral sclerosis. K811 can be used in studies related to amyotrophic lateral sclerosis.
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- CAS No.: 1355228-38-4
- Formule: C29H26N4O5
- Masse moléculaire:510.54
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Activité biologique
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
869 nM
Compound: 1; K811
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Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr
Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr
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[PMID: 31710475] |
K811 (1.0 μM; 30 min) inhibits H2O2-induced ASK1 activation in NSC34 motor neuron-like cells[1].
K811 (added 24 h after lentiviral infection and incubated until day 9 post-seeding) protects primary motor neurons from SOD1G93A-induced death in spinal cord cultures derived from E12.5 Hb9-GFP mouse embryos[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NSC34 motor neuron-like cells
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Concentration:1.0 μM
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Incubation Time:30 min (pre-incubation); 15 min (H2O2 treatment)
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Result:Significantly reduced the H2O2-induced activation of endogenous ASK1, as measured by decreased levels of phosphorylated ASK1 via immunoblotting.
| Species | Dose | Route | Tmax | Cmax | AUC0-24 |
|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | p.o. | 1.67 h | 1.27 nM/mL | 13.8 nM·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6.Cg-Tg(SOD1G93A)dl1Gur/J (male, started treatment at 28 weeks of age, SOD1G93A transgenic ALS model)[1]
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Dosage:100 mg/kg
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Administration:p.o.; daily; from 28 weeks of age until endpoint
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Result:Extended average survival time to 268.6 days, a 1.06% improvement compared to placebo.
Caused a considerable decrease in ASK1 activation in the spinal cord.
Increased the number of motor neurons in one side of the lumbar spinal cord significantly compared to placebo.
Decreased numbers of glial fibrillary acidic protein (GFAP)-positive astrocytes and ionized calcium binding adaptor molecule 1 (Iba1)-positive microglia markedly in the lumbar spinal cord compared to placebo.
Chemical Information
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CAS No. 1355228-38-4
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Masse moléculaire 510.54
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Formule C29H26N4O5
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SMILES
O=C(C1=CN(C(C)C)C2=C(C1=O)C=CC=C2)NC3=CC=C(C=C3)OC4=CN=NC5=CC(OC)=C(C=C54)OC
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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)
K811 Related Classifications
HY-182648 Related Classifications
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