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Art. -Nr.: HY-145422

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KIRA9

KIRA9 is a potent IRE1 inhibitor (IC₅₀=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.

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CAS. Nr.: 2922507-65-9
Formel: C₂₇H₂₇F₃N₆O₃S
Molecular Weight:572.60

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

KIRA9 Chemical Structure

CAS. Nr.: 2922507-65-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

KIRA9 is a potent IRE1 inhibitor (IC₅₀=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis^[1].

IC₅₀ & Target

IC₅₀: 4.8 μM (IRE1) in INS-1 cells^[1]

In Vitro

KIRA9 (0-30 μM; 2 hours) blocks the autophosphorylation induced by conditional overexpression of IRE1α in INS-1 cells (IC₅₀=4.8 μM)^[1].
KIRA9 (20 μM; 2 hours) reduces the mRNA expression of Bloc1s1, Ins1 and Ins2 in INS-1 cells^[1].
KIRA9 (20 μM; 2 hours) blunts IRE1α-dependent decay (RIDD) in ER-stressed INS-1 cells^[1].
KIRA9 (20 μM; 1 hour) markedly reduces the generation of cleaved caspase-3 and shows significant cytoprotective efficacy^[1].
KIRA9 (0-20 μM; 3 days) reduces XBP1s expression, plasma cell differentiation and IgM secretion in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:

INS-1 cells^[1]
Concentration:

20 μM
Incubation Time:

1 hour
Result:

Markedly reduced the generation of cleaved caspase-3 and showed significant cytoprotective efficacy.

Cell Differentiation Assay

Cell Line:

Mouse splenocytes (LPS-treated)^[1]
Concentration:

0, 1.25, 2.5, 5.0, 10 and 20 μM
Incubation Time:

3 days
Result:

Reduced XBP1s expression, plasma cell differentiation and IgM secretion in a dose-dependent manner.

Chemical Information

CAS. Nr. 2922507-65-9
Molecular Weight 572.60
Formel C₂₇H₂₇F₃N₆O₃S
SMILES

O=S(NC1=CC=C(OC2=NC=CC=C2C3=CC=NC(N[C@@H]4CNCCC4)=N3)C5=C1C=CC=C5)(CCC(F)(F)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Feldman HC, et al. ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR. Nat Chem Biol. 2021;17(11):1148-1156. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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