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Chemical Structure| 307543-71-1 Chemical Structure| 307543-71-1

Structure of STF-083010
CAS No.: 307543-71-1

Chemical Structure| 307543-71-1

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STF-083010 is a specific IRE1α inhibitor, inhibiting Ire1 endonuclease activity without affecting its kinase activity, following endoplasmic reticulum stress.

Synonyms: IRE1 Inhibitor I

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Product Details of STF-083010

CAS No. :307543-71-1
Formula : C15H11NO3S2
M.W : 317.38
SMILES Code : O=S(C1=CC=CS1)(/N=C/C2=C3C=CC=CC3=CC=C2O)=O
Synonyms :
IRE1 Inhibitor I
MDL No. :MFCD02332975

Safety of STF-083010

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Panc02.03 25 µM 72 h STF-083010 inhibited XBP1 splicing activity, leading to increased lysosomes and reduced viability in PDAC cells PMC6038181
primary neurons 50 μM 3 hours STF-083010 inhibited OGD-induced IRE1 phosphorylation and suppressed inflaμMasome signaling and pyroptosis PMC6412161
grass carp adipocytes 30 µM 48 hours To explore the role of the IRE1α-XBP1 signaling axis in DHA-induced adipocyte lipolysis. The results showed that STF significantly reduced the expression of IRE1α and XBP1s genes induced by DHA, and attenuated the upregulation of lipolysis-related genes (ATGL, HSLa, and HSLb) and PKA signaling pathway-related genes (GNAS, ADCY5, PRKACAb, and PRKACBa) by DHA. Additionally, STF significantly reversed the reduction of cell TG content by DHA and diminished the enhanced activity of ATGL and HSL enzymes by DHA. PMC10131065
P19 cells 5 µM 4 days To screen for small molecules that induce neuronal differentiation in P19 cells PMC164638
D3 cells 400 nM To induce neuronal differentiation in D3 cells PMC164638
CD4+ T cells 100 nM 14 days Induction of phenotypic T SCM cells, demonstrating the generation of T SCM cells PMC4776068
CD8+ T cells 100 nM 14 days Induction of phenotypic T SCM cells, demonstrating the generation of T SCM cells PMC4776068
Peripheral Blood Lymphocytes (PBLs) 1 × 10^7 PBLs 7 days Generate allogeneic antigen-specific CD8+ T SCM cells and expand in vitro PMC6286512
Primary microglia 10 μM 24 hours To investigate the modulating effect of TWS119 on microglial polarization and its underlying mechanism, results showed that TWS119 promoted the switch of microglial polarization from pro-inflaμMatory to anti-inflaμMatory phenotype via the Wnt/β-catenin signaling pathway. PMC6896312
Mouse brain microvascular endothelial cell line bEnd.3 10 μM 12 hours To evaluate the effect of TWS119 on angiogenesis in OGD-injured bEnd.3 cells, results showed that TWS119 indirectly promoted angiogenesis by modulating microglial polarization and improving the inflaμMatory microenvironment. PMC6896312
Neonatal rat cardiomyocytes (NRCMs) 1 μM 24 hours To detect SNO-Hsp90 levels, it was found that SNO-Hsp90 levels were significantly increased after Ang II treatment. PMC9343375
Neonatal rat cardiomyocytes (NRCMs) 50 μM 24 hours To detect SNO-Hsp90 levels, it was found that SNO-Hsp90 levels were significantly increased after PE treatment. PMC9343375
Human neurons 500 nM, 1 µM, 10 µM 80 minutes To test the effect of GSK3 β inhibitor TWS119 on mitochondrial function, results showed that TWS119 at 1 µM and 10 µM increased the proportion of NADH, indicating increased mitochondrial respiration PMC11485302

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Neonatal hypoxic-ischemic brain injury model Intranasal administration 7.48 µg/egg Single dose, 5 days To evaluate the short-term and long-term effects of STF-083010 on neonatal hypoxic-ischemic brain injury in rats. The results showed that STF-083010 significantly reduced brain infarct volume, improved neurological behavior, and attenuated brain atrophy. PMC5797348
rats spinal cord injury model intraperitoneal injection 75μg/kg body weight 8 injections per day, 3-times a week for 4-weeks STF-083010 inhibited SCI-induced IRE1 phosphorylation and alleviated inflammasome signaling and pyroptosis PMC6412161
mice APAP-induced liver injury model intraperitoneal injection 15 μg/pup and 45 μg/pup Single or multiple doses, lasting 2 days Investigate the protective effect of STF-083010 on APAP-induced liver injury, found that STF significantly mitigated APAP-induced liver injury and inflammation PMC8831621
Mice High-fat diet-induced diabetes model Intraperitoneal injection 10 mg/kg/d once daily until the end of the experiment STF-083010 inhibited IRE1α RNase activity, improved β-cell function, reduced inflammation, and reversed metabolic disorders. PMC11094198
mice NSG mice tail vein injection 75 mg/kg Single dose, sacrificed 24 hours later Assess the long-term survival and repopulation capacity of T SCM cells, showing that T SCM cells persist long-term in vivo and can repopulate the effector pools PMC4776068
NOD/SCID mice LCL burden mouse model Intravenous injection 30 mg/kg Twice a week for two weeks Evaluate the persistence and target cell eradication capacity of T SCM cells in vivo PMC6286512
C57BL/6 mice Permanent distal middle cerebral artery occlusion plus 1 h hypoxia model Intraperitoneal injection 200,000 cells single injection, lasting 10 weeks To investigate the effect of TWS119 on neurological recovery following experimental stroke, results showed that TWS119 ameliorated the neuroinflammatory microenvironment by modulating microglial polarization toward the anti-inflammatory phenotype, thereby facilitating neurological recovery. PMC6896312
C57BL/6J mice Transverse aortic constriction (TAC) surgery model Tail vein injection 1 × 10^7 T SCM cells Single injection, observed for 35 days To induce cardiac hypertrophy through TAC surgery, SNO-Hsp90 levels were detected, and it was found that SNO-Hsp90 levels were significantly increased after TAC surgery, and dramatically decreased in AAV9-GSNOR-treated mice. PMC9343375
Mice APPSAA/+ mice Topical application 10 mg/kg Once daily for 14 days To test the effect of TWS119 on mitochondrial activity in APPSAA/+ mice, results showed that TWS119 increased mitochondrial activity PMC11485302

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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