7-hydroxy-4-Methyl-2-oxo-2H-1-Benzopyran-8-carboxaldehyde Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

8-Formyl-4-methylumbelliferone is an inhibitor that blocks substrate access to the active site of IRE1 and selectively inactivates both Xbp1 splicing and IRE1-mediated mRNA degradation.

Allgemeine Beschreibung

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.

Biochem/physiol Actions

Cell permeable: yes

7-hydroxy-4-Methyl-2-oxo-2H-1-Benzopyran-8-carboxaldehyde Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

7-hydroxy-4-Methyl-2-oxo-2H-1-Benzopyran-8-carboxaldehyde Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29815	58
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32466	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471;	sales@sarms4muscle.com	China	10473	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3135	58
TargetMol Chemicals Inc.	+1-781-999-5354;	support@targetmol.com	United States	39040	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11680	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8615965530500	nickzhang@hangyubiotech.com	China	9948	58

14003-96-4()Verwandte Suche:

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• 2H-1-Benzopyran-8-carboxaldehyde, 7-hydroxy-4-methyl-2-oxo-
• 8C
• 7-hydroxy-4-Methyl-2-oxo-2H-1-Benzopyran-8-carboxaldehyde
• 4-Methyl-7-hydroxy-8-formylcoumarin
• 7-Hydroxy-8-formyl-4-methylcoumarin
• 8-Formyl-7-hydroxy-4-methyl-2H-1-benzopyran-2-one
• IRE1 Inhibitor III, 4μ8C
• 4M8C
• 4Μ8C (IRE1 INHIBITOR III)
• IRE1 INHIBITOR III
• IRE1 Inhibitor III, 4μ8C - CAS 14003-96-4 - Calbiochem
• 7-hydroxy-4-methyl-2-oxochromene-8-carbaldehyde
• 4mu8C
• Thioctic Acid Impurity 59
• 4μ8C, 10 mM in DMSO
• 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyd
• 4Μ8C
• 4u8C
• 8-Formyl-7-hydroxy-4-methylcoumarin
• 14003-96-4
• Inhibitors