All Photos(1)
Synonym(s):
IRE1α Inhibitor, MKC-3946, XBP1 expression blocker, MKC3946, MKC 3946
Empirical Formula (Hill Notation):
C21H20N2O3S
Recommended Products
![PERK Inhibitor I, GSK2606414 GSK2606414 is a cell-permeable, highly potent inhibitor of EIF2AK3/PERK (IC₅₀ = 0.4 nM; [ATP] = 5 µM). Targets PERK in its inactive DFG conformation at the ATP-binding region.](/deepweb/assets/sigmaaldrich/product/structures/180/559/efa716dc-d5fe-4339-a6f0-0103084fc04a/640/efa716dc-d5fe-4339-a6f0-0103084fc04a.png)
Assay
≥97% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
dark yellow
solubility
DMSO: 25 mg/mL
storage temp.
−20°C
General description
A cell-permeable compound that binds to the endoribnuclease domain of IRE1α and inhibits its activity. Blocks XBP1 mRNA splicing in RPMI 8226 human multiple myeloma cells.
A cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).
A cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IRE1
IRE1
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Mimura, N., et al. 2012. Blood.119, 5772.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service