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  6. 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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K811

K811 Chemical Structure

CAS No. : 1355228-38-4

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K811 Related Antibodies

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Description

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[1].

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 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.

K811 Related Antibodies

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 Tmax Cmax AUC0-24
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 SOD1G93A 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(SOD1G93A)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.
Molecular Weight

510.54

Formula

C29H26N4O5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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K811 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K8111355228-38-4K 811K-811spinal cord cultureslumbar spinal cordprimary motor neuronsASK1NSC34 motor neuron-like cellsamyotrophic lateral sclerosisSOD1G93A transgenic miceE12.5 Hb9-GFP mouse embryosInhibitorinhibitorinhibit

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