2. Apoptosis
  3. ASK1
  4. 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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K812

K812 Chemical Structure

CAS No. : 1355228-39-5

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K812 Related Antibodies

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Description

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[1].

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.

K812 Related Antibodies

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 Tmax Cmax AUC0-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 SOD1G93A 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.
Molecular Weight

509.55

Formula

C30H27N3O5
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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K812 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:

K8121355228-39-5K 812K-812ASK1Apoptosis signal-regulating kinase 1MAP3K5MAPKKK5Mitogen-activated protein kinase kinase kinase 5MEK kinase 5human kinasesSOD1G93A transgenic miceNSC34 motor neuron cellslumbar spinal cordglial activationmotor neuron countsamyotrophic lateral sclerosisInhibitorinhibitorinhibit

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