5.32758
IRE1α Inhibitor, MKC-3946
Synonym(s):
IRE1α Inhibitor, MKC-3946, XBP1 expression blocker, MKC3946, MKC 3946
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About This Item
Empirical Formula (Hill Notation):
C21H20N2O3S
CAS Number:
Molecular Weight:
380.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
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
SMILES string
[s]1c(ccc1C(=O)N4CCN(CC4)C)c2cc3c(c(c(cc3)O)C=O)cc2
InChI
1S/C21H20N2O3S/c1-22-8-10-23(11-9-22)21(26)20-7-6-19(27-20)15-2-4-16-14(12-15)3-5-18(25)17(16)13-24/h2-7,12-13,25H,8-11H2,1H3
InChI key
IVQVBMWPWPTSNO-UHFFFAOYSA-N
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.).
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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5327580001 | 04055977281897 |