MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α). 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.
MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α). 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.
Shipping & Handling
Shipped In
Room Temperature in continental US; may vary elsewhere
Safety & Storage
Storage Temperature
-20°C
Safety Statement
WARNING This product is not for human or veterinary use. Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
Room Temperature in continental US; may vary elsewhere
Safety & Storage
Storage Temperature
-20°C
Safety Statement
WARNING This product is not for human or veterinary use. Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
Regulatory & Compliance
We’re currently in BETA - Interested in joining? Let us know and we’ll get you set up with early access.
We’re currently in BETA - Interested in joining? Let us know and we’ll get you set up with early access.