1. MAPK/ERK Pathway
  2. p38 MAPK
  3. ASK1-IN-1

ASK1-IN-1 

Cat. No.: HY-133554
Handling Instructions

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).

For research use only. We do not sell to patients.

ASK1-IN-1 Chemical Structure

ASK1-IN-1 Chemical Structure

CAS No. : 2411382-24-4

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Description

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM)[1].

IC50 & Target

IC50: 138/21 nM (ASK1 in cell and Biochemical assays, respectively)[1]

In Vitro

ASK1-IN-1 (compound 21) has superior CYP inhibition profile and it is also inactive in a hERG assay. ASK1-IN-1 is selected for a kinase selectivity profile against a panel of 468 kinases and it is found to be moderately selective[1].

In Vivo

ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC50/IC70/IC90 at trough in the brain for 12 hours of 50/115/435 mg/kg respectively. ASK1-IN-1 has good biochemical and cellular potency, low clearance and good brain penetration in rodents[1].

Molecular Weight

405.41

Formula

C₁₉H₁₉N₉O₂

CAS No.

2411382-24-4

SMILES

COC1=NN(C2=NC=CN=C2)C=C1C(NC3=NC(C4=NN=CN4C(C)C)=CC=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

ASK1-IN-1p38 MAPKCNSpenetrantASK1MAPKbrainInhibitorinhibitorinhibit

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