STF-083010

Katalognr.S7771 Batch:S777101

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Tekniska data

Formel

C15H11NO3S2
Molekylvikt 317.38 CAS-nr. 307543-71-1
Löslighet (25°C)* In vitro DMSO 63 mg/mL (198.5 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Tillsätt lösningsmedel till produkten individuellt och i ordning.)
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 betyder svårlösligt eller olösligt.
* Vänligen notera att Selleck testar lösligheten för alla förbindelser internt, och den faktiska lösligheten kan skilja sig något från publicerade värden. Detta är normalt och beror på små variationer mellan olika partier.
* Rumstempererad frakt (Stabilitetstester visar att denna produkt kan fraktas utan några kylåtgärder.)

Beredning av stamlösningar

Biologisk aktivitet

Beskrivning STF-083010 är en specifik IRE1α-endonukleashämmare som inte påverkar dess kinasaktivitet.
Mål
IRE1α endonuclease
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.

Protokoll (från referens)

Kinasanalys:[1]
  • Cellfria IRE1-analyser

    Autofosforyleringsaktivitet bestäms genom tillsats av 32P-γ ATP. Endonukleasaktivitet bestäms genom tillsats av radiomärkt HAC1 508-nt RNA-substrat syntetiserat in vitro med hjälp av α32P-UTP. STF083010 inkuberas med rekombinant hIRE1-protein, radiomärkt HAC1 508 nt RNA och lämpliga buffertar. Kinasaktivitet kvantifieras genom polyakrylamidgelelektrofores. RNAse-klyvningsprodukter kvantifieras med 32P-γATP eller 32P-UTP-autoradiografi.
Cellanalys:[1]
  • Cellinjer

    Panc0403, Panc1005, BxPc3, and MiaPaCa2 cell lines

  • Koncentrationer

    ~50 μM

  • Inkubationstid

    ~48 h

  • Metod

    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.
Djurstudie:[1]
  • Djurmodeller

    NOD/SCID/IL2Rγ null mice

  • Doseringar

    30 mg/kg

  • Administrering

    i.p.

Referenser

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

Kundvalidering av produkt

<p>The effect of TUDCA and STF-083010 on mouse decidualization.(B) The average weight of implantation sites on day 8 under TUDCA treatment.(D) The effect of TUDCA treatment on the weight of deciduoma. (F) The average weight of implantation sites on day 8 under STF-083010 treatment. (H) The effect of STF-083010 treatment on the weight of deciduoma. (I) The effect of TUDCA on the mRNA expression of Dtprp in vitro decidualization. (J) The effect of STF-083010 on the mRNA expression of Dtprp in vitro decidualization. Data are presented as the mean ± SD, *p < 0.05.</p>

, , Mol Cell Endocrinol, 2016, 434:48-56.

Pretreatment with 50 μg STF-083010 could inhibit the up-regulation of XBP1s and XBP1u induced by chronic morphine treatment measured by western blots. (∗∗p < 0.01, ∗∗∗p < 0.001 compared with NS + vehicle group; #p < 0.05, ##p < 0.01 compared with morphine + vehicle group, n = 4 in each group). %MPE, percentage of maximal possible antinociceptive effect; NS, normal saline; STF, STF-083010; XBP1, X-box binding protein 1; XBP1s, spliced variant of XBP1; XBP1u, unspliced XBP1.

Data från [ , , Front Mol Neurosci, 2018, 11:72 ]

Effect of STF-083010, an inhibitor of IRE, on the degradation of APP induced by geniposide. After primary cortical neurons were pre-incubated with 25 μM STF083010 for 30 min, geniposide (10 μM) and high glucose (75 mM) were added and the cells were incubated for 24 h. The protein level of APP was determined by western blot. Data are shown as mean ± SD from three independent experiments. *p < 0.05, versus control (the group of 25 mM glucose); #p < 0.05 versus the group of 75 mM glucose.; &, p < 0.05 versus the group of high glucose plus geniposide.

Data från [ , , Neurochem Res, 2018, 43(3):669-680 ]

Sellecks STF-083010 Har citerats av 38 Publikationer

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

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