KIRA6

• CAT Number: I013511
• CAS Number: 1589527-65-0
• Molecular Formula: C₂₈H₂₅F₃N₆O
• Molecular Weight: 518.53
• Purity: ≥95%
• Target: IRE1
• Solubility: DMSO: 10 mM
• IUPAC Name: 1-[4-(8-amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea
• InChI: InChI=1S/C28H25F3N6O/c1-27(2,3)25-36-22(23-24(32)33-13-14-37(23)25)20-11-12-21(19-10-5-4-9-18(19)20)35-26(38)34-17-8-6-7-16(15-17)28(29,30)31/h4-15H,1-3H3,(H2,32,33)(H2,34,35,38)
• InChIKey: NOHQEAFAESMMDX-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=NC(=C2N1C=CN=C2N)C3=CC=C(C4=CC=CC=C43)NC(=O)NC5=CC=CC(=C5)C(F)(F)F

KIRA6(CAT: I013511) is a chemical compound that acts as an allosteric inhibitor of IRE1α RNase kinase activity. IRE1α is a key protein involved in the unfolded protein response (UPR), a cellular mechanism that helps maintain protein homeostasis in the endoplasmic reticulum. KIRA6 exerts its inhibitory effect by binding to an allosteric site on IRE1α, thereby interfering with its RNase kinase activity. This disruption leads to the modulation of UPR signaling and cellular stress responses. KIRA6 has been shown to have an inhibitory concentration (IC50) of approximately 0.6 µM for IRE1α RNase kinase activity, suggesting its potency in regulating this pathway.

Reference

[1]. Ghosh R, et al. Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress. Cell. 2014 Jul 31;158(3):534-48.