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Art. -Nr.: HY-182648

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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 SOD1^G93A transgenic mice. K811 extends the survival of SOD1^G93A 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. Nr.: 1355228-38-4
Formel: C₂₉H₂₆N₄O₅
Molecular Weight:510.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

K811 Chemical Structure

CAS. Nr.: 1355228-38-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	869 nM Compound: 1; K811	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	[PMID: 31710475]

In Vitro

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 SOD1^G93A-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.

Western Blot Analysis^[1]

Cell Line:

NSC34 motor neuron-like cells
Concentration:

1.0 μM
Incubation Time:

30 min (pre-incubation); 15 min (H2O2 treatment)
Result:

Significantly reduced the H2O2-induced activation of endogenous ASK1, as measured by decreased levels of phosphorylated ASK1 via immunoblotting.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-24
Mice^[1]	30 mg/kg	p.o.	1.67 h	1.27 nM/mL	13.8 nM·h/mL

In Vivo

K811 (100 mg/kg; p.o.; daily; from 28 weeks of age until endpoint) extends the survival of SOD1^G93A transgenic mice by 1.06%, inhibits spinal cord ASK1 activation, preserves motor neurons, and reduces glial activation^[1].

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

Animal Model:

B6.Cg-Tg(SOD1^G93A)dl1Gur/J (male, started treatment at 28 weeks of age, SOD1G93A transgenic ALS model)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; daily; from 28 weeks of age until endpoint
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

CAS. Nr. 1355228-38-4
Molecular Weight 510.54
Formel C₂₉H₂₆N₄O₅
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Fujisawa T, et al. The ASK1-specific inhibitors K811 and K812 prolong survival in a mouse model of amyotrophic lateral sclerosis. Hum Mol Genet. 2016;25(2):245-253. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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