5.32758
IRE1α Inhibitor, MKC-3946
别名:
IRE1α Inhibitor, MKC-3946, XBP1 expression blocker, MKC3946, MKC 3946
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关于此项目
经验公式（希尔记法）:
C21H20N2O3S
化学文摘社编号:
分子量:
380.46
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
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)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable