| Name | STF-083010 |
| Description | STF-083010 is a selective inhibitor of the IRE1α endonuclease. |
| Cell Research | 3×10E3 (Panc0403, Panc1005, BxPc3, and MiaPaCa2) cell lines are seeded in 96-well plates overnight, and STF-083010(~50 μM) treatment for 48 hours started the next day. |
| Kinase Assay | Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography. |
| Animal Research | NOD/SCID/IL2Rγ null mice were injected intraperitoneally of STF-083010(30 mg/kg) dissolved in 16% chremophor. |
| In vitro | WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 hours cultures. In MM.1R MM, MM.1S, and RPMI 8226 cell lines, STF-083010 displays cytostatic and cytotoxic activity in a dose and time-dependent manner. In Eμ-TCL1 CLL cells, STF-083010 displays about 70% growth inhibition after 3 days culture. In SU8686, Panc0403, and MiaPaCa2 cell lines, STF-083010 blocks IRE1α's endonuclease and inhibits XBP1 splicing activity without affecting its kinase activity. |
| In vivo | STF-083010 (i.p., 30 mg/kg) signi?cantly inhibits the growth of the tumor in human multiple myeloma (MM) xenografts model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 40 mg/mL (126.03 mM)
|
| Keywords | STF 083010 | Inositol requiring enzyme 1 | Inhibitor | inhibit | IRE1 | STF-083010 |
| Inhibitors Related | B I09 | Sunitinib | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | Sunitinib Malate | D-F07 | MKC8866 | APY29 | GSK2850163 (S enantiomer) | 4μ8C | GSK2850163 | Toyocamycin | IXA4 |
| Related Compound Libraries | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Anti-Diabetic Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library |
United States
