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Art. -Nr.: HY-183933

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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 SOD1^G93A transgenic mice. K812 can be used for the research of amyotrophic lateral sclerosis.

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CAS. Nr.: 1355228-39-5
Formel: C₃₀H₂₇N₃O₅
Molecular Weight:509.55

Speicherung:

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

K812 Chemical Structure

CAS. Nr.: 1355228-39-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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	277 nM Compound: 2; K812	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

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.

Western Blot Analysis^[1]

Cell Line:

NSC34 motor neuron cells
Concentration:

1.0 μM
Incubation Time:

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

Significantly reduced H₂O₂-induced phosphorylation of endogenous ASK1 in NSC34 cells, as detected by immunoblotting.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t
Mice^[1]	30 mg/kg	p.o.	2.00 h	4.80 nM/mL	73.9 nM·h/mL

In Vivo

K812 (30 mg/kg; p.o.; daily; from 28 weeks of age until study endpoint) extends the survival of SOD1^G93A transgenic mice by 1.08%, reduces ASK1 activation in the spinal cord, preserves motor neuron counts, and inhibits 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, 28 weeks of age at treatment start, ALS transgenic model)^[1]
Dosage:

30 mg/kg
Administration:

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

CAS. Nr. 1355228-39-5
Molecular Weight 509.55
Formel C₃₀H₂₇N₃O₅
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
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.

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100 mg

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