Home ER stress & UPR IRE1 inhibitor STF-083010 For research use only.

STF-083010

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

STF-083010 Chemical Structure

STF-083010 Chemical Structure

CAS No. 307543-71-1

Purity & Quality Control

STF-083010 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF21 cell Function assay Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=9.939 μM 24749861
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Biological Activity

Description STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity.
Targets
IRE1α endonuclease [1]
In vitro
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell count 29423023
In Vivo
In vivo In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor. [1]
Animal Research Animal Models NOD/SCID/IL2Rγ null mice
Dosages 30 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 317.38 Formula

C15H11NO3S2
CAS No. 307543-71-1 SDF Download STF-083010 SDF
Smiles C1=CC=C2C(=C1)C=CC(=C2C=NS(=O)(=O)C3=CC=CS3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (198.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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