IRE1α kinase-IN-1
CAS No. 2328097-41-0
IRE1α kinase-IN-1 ( —— )
Catalog No. M28763 CAS No. 2328097-41-0
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 335 | Get Quote |
|
10MG | 500 | Get Quote |
|
25MG | 806 | Get Quote |
|
50MG | 1098 | Get Quote |
|
100MG | 1485 | Get Quote |
|
200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameIRE1α kinase-IN-1
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NoteResearch use only, not for human use.
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Brief DescriptionIRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform.
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DescriptionIRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).(In Vitro):IRE1α kinase-IN-1 (compound 31) prevents endoplasmic reticulum stress-induced IRE1α oligomerization and phosphorylation, and inhibits endoribonuclease activity in human cells.IRE1α kinase-IN-1 and is very high selectivity with >70% inhibition of only 4/455 kinases. IRE1α kinase-IN-1 inhibits recombinant G547 IRE1α KEN domain pS274 autophosphorylation with an IC50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC50 of 0.27 μM.IRE1α kinase-IN-1 inhibits both tunicamycin- and thapsigargin-induced IRE1α-dependent splicing of XBP1 luciferase fusion mRNA in HEK293 cells with IC50s ranging 0.68-1.63 μM.IRE1α kinase-IN-1 (0-20 μM) inhibits IRE1α-dependent XBP1s mRNA expression in H929 cells.IRE1α kinase-IN-1 (0-20 μM) dose-dependently inhibits tunicamycin-induced expression of XBP1s in NCI-H929 cells.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorAntibacterial
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Research Area——
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Indication——
Chemical Information
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CAS Number2328097-41-0
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Formula Weight505.0
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Molecular FormulaC26H26ClFN8
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Purity>98% (HPLC)
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Solubility——
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SMILESCN1CCC(CNc2cc(Cl)nn3c2ncc3-c(cc2nc(Nc3ccccc3)[nH]c2c2)c2F)CC1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Lo Re V 3rd, et al. Oral Azole Antifungal Medications and Risk of Acute Liver Injury, Overall and by Chronic Liver Disease Status. Am J Med. 2016 Mar;129(3):283-91.e5.
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