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IRE1α kinase-IN-1 - 99%, high purity , CAS No.2328097-41-0

    Grade & Purity:
  • ≥99%
In stock
Item Number
I647598
Grouped product items
SKU Size
Availability
Price Qty
I647598-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
I647598-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$800.90
I647598-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,650.90

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC 50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphoryl
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC 50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC 50 =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 IC 50 of 160 nM. IRE1α kinase-IN-1 inhibits tunicamycin-induced GFP-IRE1α foci in HEK293 cells with an IC 50 of 0.74 μM. IRE1α kinase-IN-1 Inhibits ATP-site LanthaScreen tracer binding to recombinant dephosphorylated G547 IRE1α KEN with an IC 50 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 IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Names and Identifiers

Smiles CN1CCC(CNC2=CC(Cl)=NN3C2=NC=C3C4=C(F)C=C5C(N=C(NC6=CC=CC=C6)N5)=C4)CC1
Molecular Weight 504.99

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 25 mg/mL (49.51 mM; ultrasonic and warming and heat to 60°C)

Solution Calculators

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