STF-083010

Catalog No.S7771

STF-083010 Chemical Structure

Molecular Weight(MW): 317.38

STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.

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Cited by 4 Publications

3 Customer Reviews

  • 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

Biological Activity

Description STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Targets
IRE1α endonuclease [1]
In vitro

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. [1] [2] In MiaPaCa2, Panc0403, and SU8686 cell lines, STF-083010 inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity. [1] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF21 cell NGjQN2tHfW6ldHnvckBie3OjeR?= M4fIUWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRicIXybZRqdi2KaYOteIFo\2WmIFnSSU0yKFKQYYPlJIV5eHKnc4Pl[EBqdiCVRkKxJINmdGy|IIXzbY5oKFiEUD2xJHJPSSC|dHXtJIxwd3BiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOiCqcoOgZpkhTlKHVD3zeZBxemW|c3nvckBie3OjeTygTWM2OD17LkmzPUDPxE1? MkP6NlQ4PDl6NkG=

... Click to View More Cell Line Experimental Data

In vivo In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor. [1]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: Panc0403, Panc1005, BxPc3, and MiaPaCa2 cell lines
  • Concentrations: ~50 μM
  • Incubation Time: ~48 h
  • Method: Three thousand cells are seeded in 96-well plates overnight and drug treatment started the next day. After 48 h incubation, MTT is added to cells and cultured at 37℃ for 4 h followed by stop solution (4 mM HCl, 0.1% Nondet P40 in isopropanol) which is added to dissolve MTT. The plates are read with a spectrophotometer at 590 nm absorbance with reference at 630 nm. IC50 values are calculated using GraphPad Prism.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: NOD/SCID/IL2Rγ null mice
  • Formulation: 16% chremophor
  • Dosages: 30 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (198.5 mM)
Water Insoluble
Ethanol Insoluble
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.
2mg/mL

* 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.

Chemical Information

Molecular Weight 317.38
Formula

C15H11NO3S2

CAS No. 307543-71-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID