Kira8 (Ire-1 inhibitor, AMG-18) is a monoselective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

 

Brand: BCM

 

Target: IRE1

 

Signaling Pathways: Cell Cycle/Checkpoint

 

In Vitro: Kira8 more effectively causes IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. Kira8 blocks IRE1α oligomerization and effectively inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs.

 

Boiling Point: 812.6±75.0 °C(Predicted)

 

pKa: 7.66±0.30(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: CC1=C(C2=C(C=C1)C(=CC=C2)NS(=O)(=O)C3=CC=CC=C3Cl)OC4=C(C=CC=N4)C5=NC(=NC=C5)N[C@H]6CCCNC6  

 

InChIKey: XMWUCMFVDXDRDE-NRFANRHFSA-N  

 

InChI: InChI=1S/C31H29ClN6O3S/c1-20-13-14-22-23(8-4-11-27(22)38-42(39,40)28-12-3-2-10-25(28)32)29(20)41-30-24(9-6-17-34-30)26-15-18-35-31(37-26)36-21-7-5-16-33-19-21/h2-4,6,8-15,17-18,21,33,38H,5,7,16,19H2,1H3,(H,35,36,37)/t21-/m0/s1

 

Attribute
[Chem Name]	2-chloro-N-[6-methyl-5-[3-[2-[[(3S)-piperidin-3-yl]amino]pyrimidin-4-yl]pyridin-2-yl]oxynaphthalen-1-yl]benzenesulfonamide
[Synonym]	Kira8; Ire-1 inhibitor; AMG-18
[CAS No.]	1630086-20-2
[MDL No.]	MFCD28404657
[Formula]	C31H29ClN6O3S
[Molecular]	601.12
[Form]	Solid Powder
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

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