AK177 

AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively. AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity^[1].

AK177 inhibits PDGFRA kinase activity in cell-free HTRF assays with an IC₅₀ of 9.0 nM^[1].
AK177 inhibits KIT kinase activity with an IC₅₀ of 113.7 nM in a cell-free HTRF assay^[1].
AK177 inhibits the activity of 49 out of 85 tested kinases in a cell-free kinome profiling assay^[1].
AK177 (0.25-20 μM; 24 h) weakly induces XBP1 mRNA splicing in MCF-7 cells, with an activation fold change of less than 2 after treatment with 20 μM for 24 h^[1].
AK177 (0.25-20 μM; 24 h) does not induce detectable Bloc1s1 mRNA degradation via RIDD in MCF-7 cells, even at the highest treatment concentration of 20 μM for 24 h^[1].
AK177 (1-100 μM; 72 h) exerts no significant inhibitory effect on the viability of HT-29, MDA-MB-231 and MCF-7 cells even at concentrations up to 100 μM following 72 h of treatment^[1].

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

564.62

C₂₆H₂₈N₈O₅S

CC1=CC(NC2=CC(N3CCN(CC3)C(C4=CC=CC=C4)C(O)=O)=NC(OC5=CC=C(C=C5)S(N)(=O)=O)=N2)=NN1

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• [1]. Avathan Veettil AK, et al. Pyrazolylpyrimidinamines Decorated via Petasis Reaction as Small-Molecule Activators of the RNA-Degrading Ribonuclease IRE1α. ACS Bio & Med Chem Au. 2026 Feb 27.