412512
4μ8C
≥95% (HPLC), selective inhibitor of IRE1α, powder
동의어(들):
IRE1 Inhibitor III, 4μ8C, 8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde, ER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C11H8O4
CAS 번호:
Molecular Weight:
204.18
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
제품 이름
IRE1 Inhibitor III, 4μ8C, IRE1 Inhibitor III, CAS 14003-96-4, is a cell-permeable. Covalent inhibitor of IRE1 RNase activity (IC50 = 550 and 45 nM, respectively, with 0 & 16 min preincubation in RNA cleavage assays).
SMILES string
O=C(C=C1C)OC2=C1C=CC(O)=C2C=O
InChI key
RTHHSXOVIJWFQP-UHFFFAOYSA-N
InChI
1S/C11H8O4/c1-6-4-10(14)15-11-7(6)2-3-9(13)8(11)5-12/h2-5,13H,1H3
assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 25 mg/mL
shipped in
ambient
Quality Level
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General description
A cell-permeable coumarin o-hydroxyaldehyde compound that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50 = 550, 230, 180, 100, and 45 nM, respectively, with 0, 2, 4, 8, 16, min drug preincubation in FRET-based RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50 = 6.9 and 4.1 µM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin (Cat. No. 654380) treatment. Also demonstrated to inhibit ER capacity expansion (Effective conc. 32 µM) and amylase secretion (IC50<2 µM) upon stress induction by Dexamethasone (Cat. No. 265005) treatment in rat AR42J tumoral acinar pancreatic cells. Structural analysis reveals that the reduced water accessibility to Lys907 in IRE1 native conformation accounts for the unusual stability of Lys907 Schiff base formation and forms the basis of selective IRE1 RNase inhibition by 4μ8C and STF083010 (Cat. No. 412510). Although 4μ8C, but not STF083010, is also shown to inhibit IRE1 autophosphorylation by Schiff base formation with IRE1 Lys599 in the absence of ADP, cellular nucleotide prevents 4μ8C from targeting IRE1 Lys599 and inhibiting IRE1 kinase activity intracellularly.
A cell-permeable coumarin o-hydroxyaldehyde that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50 = 550 and 45 nM, respectively, with 0 and 16 min drug preincubation in RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50 = 6.9 and 4.1 µM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin (Cat. No. 654380) treatment. Comparing to STF083010 (Cat. No. 412510), 4μ8C is also shown to inhibit IRE1 autophosphorylation in cell-free assays via Schiff base formation with IRE1 Lys599 in the absence of ADP, however cellular nucleotide prevents 4μ8C from targeting IRE1 Lys599 intracellularly.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IRE1
IRE1
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months.
Other Notes
Cross, B.C.S., et al. 2012. Proc. Natl. acad. Sci. USA109, E869.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
HIF1I?-dependent hypoxia response in myeloid cells requires IRE1I?.
Mawambo, et al.
Journal of Neuroinflammation, 20, 145-145 (2023)
Stefanie Marek-Iannucci et al.
JCI insight, 7(6) (2022-02-16)
Kawasaki disease (KD) is the leading cause of noncongenital heart disease in children. Studies in mice and humans propound the NLRP3/IL-1β pathway as the principal driver of KD pathophysiology. Endoplasmic reticulum (ER) stress can activate the NLRP3 inflammasome, but the
Aparajita Madhavan et al.
Nature communications, 13(1), 608-608 (2022-02-03)
In obesity, signaling through the IRE1 arm of the unfolded protein response exerts both protective and harmful effects. Overexpression of the IRE1-regulated transcription factor XBP1s in liver or fat protects against obesity-linked metabolic deterioration. However, hyperactivation of IRE1 engages regulated IRE1-dependent
Methionine consumption by cancer cells drives a progressive upregulation of PD-1 expression in CD4 T cells.
Pandit, et al.
Nature Communications, 14, 2593-2593 (2023)
Mariana Marques et al.
iScience, 27(3), 109100-109100 (2024-02-26)
Influenza A virus (IAV) employs multiple strategies to manipulate cellular mechanisms and support proper virion formation and propagation. In this study, we performed a detailed analysis of the interplay between IAV and the host cells' proteostasis throughout the entire infectious
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 412512-25MGCN | 04055977188189 |
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