STF 083010 (Synonyms: IRE1 Inhibitor I) |
رقم الكتالوجGC12937
One-Click Copy Product Info
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STF 083010 هو مثبط محدد لـ IRE1α. يثبط STF 083010 نشاط نوكلياز Ire1 ، دون التأثير على نشاط كينازه ، بعد إجهاد الشبكة الإندوبلازمية.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 307543-71-1
Sample solution is provided at 25 µL, 10mM.
STF 083010 is an inhibitor of endonuclease activity of Inositol requiring-enzyme 1α (IRE1α) with an IC50 value of 9.94µM for IRE-1 RNase[1]. STF 083010 specifically targets the IRE1-XBP1 axis, blocking the IRE1 activity after endoplasmic reticulum stress, interfering with the splicing of endogenous XBP1 mRNA and inhibiting the production of active sXBP1 protein[2]. STF 083010 has been widely used in cancer research to inhibit the growth of various cancer cells and reverse drug resistance[3].
In vitro, STF 083010 treatment (60µM) for 24 hours significantly reduced the maximum mitochondrial respiratory rate and reserve respiratory capacity of SH-SY5Y cells[4]. Treatment with 80µM STF 083010 for 24 hours alleviated the CdCl2-induced autophagy in GC-2spd cells, resulting in a significant decrease in the protein expression levels of autophagy-related proteins LC3-II/LC3-I and Beclin-1[5].
In vivo, a single intraperitoneal injection of STF 083010 (50mg/kg) 2 hours before thioacetamide (TAA) administration alleviated TAA-induced acute liver injury, attenuated oxidative stress, and reduced inflammation in mice within 24 hours[6]. Intraperitoneal injection of 30mg/kg dose of STF 083010, twice a week for 3 weeks, alleviated liver fibrosis induced by carbon tetrachloride in mice and promoted the upregulation of miR-122 expression[7]. Intraperitoneal injection of STF 083010 at a dose of 30mg/kg/day for 3 days alleviated the lung injury elicited by lipopolysaccharide (LPS) in mice and restored the expression of β-catenin in airway epithelial cells[8].
References:
[1] Ranatunga S, Tang C H A, Kang C W, et al. Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity[J]. Journal of medicinal chemistry, 2014, 57(10): 4289.
[2] Papandreou I, Denko N C, Olson M, et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma[J]. Blood, The Journal of the American Society of Hematology, 2011, 117(4): 1311-1314.
[3] Ming J, Ruan S, Wang M, et al. A novel chemical, STF-083010, reverses tamoxifen-related drug resistance in breast cancer by inhibiting IRE1/XBP1[J]. Oncotarget, 2015, 6(38): 40692.
[4] Hatokova Z, Evinova A, Racay P. STF-083010 an inhibitor of IRE1α endonuclease activity affects mitochondrial respiration and generation of mitochondrial membrane potential[J]. Toxicology in Vitro, 2023, 92: 105652.
[5] Han Y, Dai J, Cheng J, et al. Cadmium induces autophagy via IRE1 signaling pathway activated by Ca2+ in GC-2spd cells[J]. Reproductive Toxicology, 2025, 135: 108950.
[6] Zhan F, Zhao G, Li X, et al. Inositol-requiring enzyme 1 alpha endoribonuclease specific inhibitor STF-083010 protects the liver from thioacetamide-induced oxidative stress, inflammation and injury by triggering hepatocyte autophagy[J]. International Immunopharmacology, 2019, 73: 261-269.
[7] Chen Q Q, Zhang C, Qin M Q, et al. Inositol-requiring enzyme 1 alpha endoribonuclease specific inhibitor STF-083010 alleviates carbon tetrachloride induced liver injury and liver fibrosis in mice[J]. Frontiers in Pharmacology, 2018, 9: 1344.
[8] Zhang H, Li J, Wang X, et al. IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury[J]. Pulmonary Pharmacology & Therapeutics, 2023, 83: 102263.
| Cell experiment [1]: | |
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Cell lines |
L02 cells |
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Preparation Method |
L02 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in a 96-well plate at a density of 2×103 cells/well overnight, and were pre-treated with or without Salidroside (10µM) or STF 083010 (50µM) for 6h, then followed by hypoxia. For experimental hypoxia, cells were incubated with the serum-free medium and placed in an airtight humidified chamber at 37°C, 5% CO2, and 95% N2. The corresponding normoxia control cells were cultured in a humidified incubator with 37°C, 5% CO2, and 21% O2. p-JNK, BAX, and cleaved caspase 12 and 9 protein expression levels were measured. |
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Reaction Conditions |
50µM; 6h |
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Applications |
STF 083010 treatment reversed the inhibitory effect of Salidroside on the protein expression of pJNK, BAX, cleaved caspase 12 and 9 in L02 cells under hypoxic conditions. |
| Animal experiment [2]: | |
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Animal models |
Male BALB/c mice |
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Preparation Method |
Male C57BL/6 mice (6 weeks old; 20-22g) were housed in a specific pathogen-free facility at controlled temperature/humidity (23°C±2°C/50%±10%) with a 12h dark/light cycle (lighting 7:00-19:00), with free access to water and food. After a week of acclimatization, a murine model of Acute lung injury (ALI) was established by intratracheal instillation of 5mg/kg LPS. Mice were randomly divided into the following 3 groups (n=10/group): control group, LPS group, LPS + STF 083010 group. STF 083010 (30mg/kg in 0.1% DMSO diluted with PBS), was injected intraperitoneally immediately after LPS instillation once a day for a consecutive of three days. Control mice were treated in a similar manner with the same volume of vehicle for comparison. The mice were sacrificed 72h after LPS instillation. Lung tissues of mice were collected for analysis. |
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Dosage form |
30mg/kg/day; 3 days; i.p. |
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Applications |
STF 083010 treatment significantly attenuated LPS-induced lung injury and inflammation in mice. |
References: [1] Xiong Y, Wang Y, Xiong Y, et al. Salidroside alleviated hypoxia-induced liver injury by inhibiting endoplasmic reticulum stress-mediated apoptosis via IRE1α/JNK pathway[J]. Biochemical and biophysical research communications, 2020, 529(2): 335-340. [2] Zhang H, Li J, Wang X, et al. IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury[J]. Pulmonary Pharmacology & Therapeutics, 2023, 83: 102263. | |
| Cas No. | 307543-71-1 | SDF | |
| المرادفات | IRE1 Inhibitor I | ||
| Chemical Name | (Z)-N-((2-oxonaphthalen-1(2H)-ylidene)methyl)thiophene-2-sulfonamide | ||
| Canonical SMILES | O=S(N/C=C1C2=CC=CC=C2C=CC/1=O)(C3=CC=CS3)=O | ||
| Formula | C15H11NO3S2 | M.Wt | 317.38 |
| الذوبان | ≥ 31.7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1508 mL | 15.754 mL | 31.508 mL |
| 5 mM | 630.2 μL | 3.1508 mL | 6.3016 mL |
| 10 mM | 315.1 μL | 1.5754 mL | 3.1508 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)