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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C15H11NO3S2 |
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分子量 | 317.38 | CAS No. | 307543-71-1 | |
Solubility (25°C)* | 体外 | DMSO | 63 mg/mL (198.5 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity. |
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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] |
in vivo | In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor. [1] |
キナーゼアッセイ | Cell free IRE1 assays | |
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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. | ||
細胞アッセイ | 細胞株 | Panc0403, Panc1005, BxPc3, and MiaPaCa2 cell lines |
濃度 | ~50 μM | |
反応時間 | ~48 h | |
実験の流れ | 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. | |
動物実験 | 動物モデル | NOD/SCID/IL2Rγ null mice |
投薬量 | 30 mg/kg | |
投与方法 | i.p. |
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, , Mol Cell Endocrinol, 2016, 434:48-56.
Data from [Data independently produced by , , Front Mol Neurosci, 2018, 11:72]
Data from [Data independently produced by , , Neurochem Res, 2018, 43(3):669-680]
Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31] | PubMed: 38212315 |
HRS mediates tumor immune evasion by regulating proteostasis-associated interferon pathway activation [ Cell Rep, 2023, 10.1016/j.celrep.2023.113352] | PubMed: 37948180 |
Acute Endoplasmic Reticulum Stress Suppresses Hepatic Gluconeogenesis by Stimulating MAPK Phosphatase 3 Degradation [ Int J Mol Sci, 2023, 24(21)15561] | PubMed: 37958545 |
Emodin, an Emerging Mycotoxin, Induces Endoplasmic Reticulum Stress-Related Hepatotoxicity through IRE1α-XBP1 Axis in HepG2 Cells [ Toxins (Basel), 2023, 15(7)455] | PubMed: 37505724 |
Emodin, an Emerging Mycotoxin, Induces Endoplasmic Reticulum Stress-Related Hepatotoxicity through IRE1α-XBP1 Axis in HepG2 Cells [ Toxins (Basel), 2023, 15(7)455] | PubMed: 37505724 |
IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Pulm Pharmacol Ther, 2023, 10.1016/j.pupt.2023.102263] | PubMed: 37935327 |
UPF3B modulates endoplasmic reticulum stress through interaction with inositol-requiring enzyme-1α [ Research Square, 2023, ] | PubMed: none |
Scleral PERK and ATF6 as targets of myopic axial elongation of mouse eyes [ Nat Commun, 2022, 13(1):5859] | PubMed: 36216837 |
Pharmacologic IRE1/XBP1s activation promotes systemic adaptive remodeling in obesity [ Nat Commun, 2022, 13(1):608] | PubMed: 35105890 |
Tp47 promoted the phagocytosis of HMC3 cells though autophagy induced by endoplamic reticlum stress [ J Eur Acad Dermatol Venereol, 2022, 10.1111/jdv.18295] | PubMed: 35666816 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。