An inhibitor of IRE1α; inhibits ER stress induced XBP1 splicing and reduces expression of the XBP1 target genes SEC61A1

MKC-3946 – 5 mg

Brand:
Cayman
CAS:
1093119-54-0
Storage:
-20
UN-No:
Non-Hazardous - /

MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α).{41446} It inhibits basal XBP1 splicing, a marker of IRE1α activity, in RPMI 8226 multiple myeloma cells in a concentration-dependent manner. MKC-3946 also inhibits XBP1 splicing induced by endoplasmic reticulum (ER) stress and reduces expression of the XBP1 target genes SEC61A1, p58IPK, and ERdj4 in RPMI 8226 cells. In vitro, it is cytotoxic to multiple myeloma cell lines but has no effect on normal mononuclear cells. In vivo, MKC-3946 (100 mg/kg) reduces tumor growth and XBP1 splicing in an RPMI 8226 mouse xenograft model.  

 

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Description

An inhibitor of IRE1α; inhibits ER stress induced XBP1 splicing and reduces expression of the XBP1 target genes SEC61A1, p58IPK, and ERdj4 in RPMI 8226 cells; cytotoxic to multiple myeloma cell lines but has no effect on normal mononuclear cells; reduces tumor growth and XBP1 splicing in an RPMI 8226 mouse xenograft model (100 mg/kg)

Formal name: 2-hydroxy-6-[5-[(4-methyl-1-piperazinyl)carbonyl]-2-thienyl]-1-naphthalenecarboxaldehyde

Synonyms: 

Molecular weight: 380.5

CAS: 1093119-54-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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