K812
K812 is an orally active ASK1 inhibitor with a 6 nM IC50 against ASK1. K812 selectively inhibits ASK1 activation. K812 inhibits glial activation in the lumbar spinal cord. K812 extends survival of SOD1G93A transgenic mice. K812 can be used for the research of amyotrophic lateral sclerosis.
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- CAS No.: 1355228-39-5
- Formule: C30H27N3O5
- Masse moléculaire:509.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
277 nM
Compound: 2; K812
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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] |
K812 is a selective inhibitor of ASK1, with an IC50 of 6 nM for ASK1[1].
K812 (1.0 μM; 30 min pre-incubation) inhibits H2O2-induced ASK1 activation in NSC34 motor neuron cells[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 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 H2O2-induced phosphorylation of endogenous ASK1 in NSC34 cells, as detected by immunoblotting.
| Species | Dose | Route | Tmax | Cmax | AUC0-t |
|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | p.o. | 2.00 h | 4.80 nM/mL | 73.9 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(SOD1*G93A)dl1Gur/J (male, 28 weeks of age at treatment start, ALS transgenic model)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; from 28 weeks of age until study endpoint
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Result:Extended average survival time to 273.3 days, representing a 1.08% improvement compared to placebo.
Caused a considerable decrease in ASK1 activation in the spinal cord relative to placebo-treated mice.
Increased the number of motor neurons in the lumbar spinal cord significantly compared to placebo-treated mice.
Decreased numbers of GFAP-positive astrocytes and Iba1-positive microglia markedly in the lumbar spinal cord compared to placebo-treated mice.
Chemical Information
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CAS No. 1355228-39-5
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Masse moléculaire 509.55
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Formule C30H27N3O5
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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=C5C=C(OC)C(OC)=CC5=NC=C4
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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)
K812 Related Classifications
HY-183933 Related Classifications
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