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.
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- Fòrmula: C26H28N8O5S
- Peso molecular:564.62
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:0.25, 0.77, 2.22, 6.67 and 20 μM
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Incubation Time:24 h
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Result:Induced less than 2-fold increase in XBP1s mRNA levels at the highest tested concentration of 20 μM, with minimal concentration-dependent changes across all tested doses.\nDid not cause significant changes in Bloc1s1 mRNA levels at any tested concentration.
Chemical Information
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Peso molecular 564.62
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Fòrmula C26H28N8O5S
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SMILES
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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AK177 Related Classifications
HY-181886 Related Classifications
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