For research use only.
CAS No. 307543-71-1
STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Selleck's STF-083010 has been cited by 13 publications
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The effect of TUDCA and STF-083010 on mouse decidualization.(B) The average weight of implantation sites on day 8 under TUDCA treatment.(D) The effect of TUDCA treatment on the weight of deciduoma. (F) The average weight of implantation sites on day 8 under STF-083010 treatment. (H) The effect of STF-083010 treatment on the weight of deciduoma. (I) The effect of TUDCA on the mRNA expression of Dtprp in vitro decidualization. (J) The effect of STF-083010 on the mRNA expression of Dtprp in vitro decidualization. Data are presented as the mean ± SD, *p < 0.05.
Mol Cell Endocrinol, 2016, 434:48-56.. STF-083010 purchased from Selleck.
Pretreatment with 50 μg STF-083010 could inhibit the up-regulation of XBP1s and XBP1u induced by chronic morphine treatment measured by western blots. (∗∗p < 0.01, ∗∗∗p < 0.001 compared with NS + vehicle group; #p < 0.05, ##p < 0.01 compared with morphine + vehicle group, n = 4 in each group). %MPE, percentage of maximal possible antinociceptive effect; NS, normal saline; STF, STF-083010; XBP1, X-box binding protein 1; XBP1s, spliced variant of XBP1; XBP1u, unspliced XBP1.
Front Mol Neurosci, 2018, 11:72. STF-083010 purchased from Selleck.
Effect of STF-083010, an inhibitor of IRE, on the degradation of APP induced by geniposide. After primary cortical neurons were pre-incubated with 25 μM STF083010 for 30 min, geniposide (10 μM) and high glucose (75 mM) were added and the cells were incubated for 24 h. The protein level of APP was determined by western blot. Data are shown as mean ± SD from three independent experiments. *p < 0.05, versus control (the group of 25 mM glucose); #p < 0.05 versus the group of 75 mM glucose.; &, p < 0.05 versus the group of high glucose plus geniposide.
Neurochem Res, 2018, 43(3):669-680. STF-083010 purchased from Selleck.
Purity & Quality Control
Choose Selective IRE1 Inhibitors
|Description||STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.|
In RPMI 8226, MM.1S, and MM.1R MM cell lines, STF-083010 exhibits cytostatic and cytotoxic activity in a dose and time dependent manner.   In MiaPaCa2, Panc0403, and SU8686 cell lines, STF-083010 inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity.  In Eμ-TCL1 CLL cells, STF-083010 exhibits about 70% growth inhibition after 3 days culture. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 h. WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. 
|In vivo||In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) signiﬁcantly inhibits the growth of tumor. |
Cell free IRE1 assays:Autophosphorylation activity is determined by the addition of 32P-γ ATP. Endonuclease activity is determined by the addition of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. STF083010 is incubated with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography.
|In vitro||DMSO||63 mg/mL (198.5 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40%PEG 300+5% Tween80 +ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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