STF-083010

製品コードS7771 バッチS777102

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H11NO3S2
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 STF-083010 は、IRE1αのキナーゼ活性に影響を与えることなく、その特異的なIRE1αエンドヌクレアーゼを阻害します。
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. In MiaPaCa2, Panc0403, and SU8686 cell lines, this compound inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity. In Eμ-TCL1 CLL cells, it exhibits about 70% growth inhibition after 3 days culture. In MEC1 and MEC2 cells, this chemical produces 20% growth inhibition in 48 h. WaC3 cells respond to treatments with this compound with gradually decreased growth.
in vivo In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/21081713/
  • https://pubmed.ncbi.nlm.nih.gov/24952679/
  • https://pubmed.ncbi.nlm.nih.gov/22692508/

カスタマーフィードバック

, , 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

α-Synuclein orchestrates Th17 responses as antigen and adjuvant in Parkinson's disease [ J Neuroinflammation, 2025, 22(1):38] PubMed: 39934862
The Protective Role of the IRE1α/XBP1 Signaling Cascade in Autophagy During Ischemic Stress and Acute Kidney Injury [ Cell Stress Chaperones, 2025, S1355-8145(25)00010-0] PubMed: 39983812
UPF3B modulates endoplasmic reticulum stress through interaction with inositol-requiring enzyme-1α [ Cell Death Dis, 2024, 15(8):587] PubMed: 39138189
Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31] PubMed: 38212315
HSP47 Increases the Expression of Type I Collagen in Fibroblasts through IRE1α Activation, XBP1 Splicing, and Nuclear Translocation of β-Catenin [ Cells, 2024, 13(6)527] PubMed: 38534372
Kaempferol attenuates particle-induced osteogenic impairment by regulating ER stress via the IRE1α-XBP1s pathway [ J Biol Chem, 2024, 300(6):107394] PubMed: 38768813
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
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

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。

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