1. Cell Cycle/DNA Damage
  2. IRE1

STF-083010 

Cat. No.: HY-15845 Purity: >98.0%
Handling Instructions

STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

For research use only. We do not sell to patients.

STF-083010 Chemical Structure

STF-083010 Chemical Structure

CAS No. : 307543-71-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
Estimated Time of Arrival: December 31
100 mg USD 504 In-stock
Estimated Time of Arrival: December 31
200 mg USD 888 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Top Publications Citing Use of Products

    STF-083010 purchased from MCE. Usage Cited in: Exp Anim. 2018 Jul 30;67(3):373-382.

    Effect of STF-083010 administration on endoplasmic reticulum (ER) stress of acute renal failure (ARF) kidneys.

    STF-083010 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    IRE1 kinase activity inhibitor represses JNK activation induced by viral infection in HEC-1-A cells. HEC-1-A cells were pretreated or mock-pretreated with APY29, only or both APY29, and STF-083010 for 30 min and then infected or mock-infected with HSV-1.

    STF-083010 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    HEC-1-A cells are pretreated or mockpretreated with Tg for 30 min then mock-infected or infected with HSV-1 or treated with STF-083010. Total cellular RNA is extracted after 12 h p.i. and the mRNA levels are determined by real-time PCR.

    STF-083010 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    Inhibition of IRE1 kinase activity has an inhibitory effect on HSV-1 replication in HEC-1-A cells. Cells are presence or absence of APY29 or STF-083010 or both of two drugs and then infected with HSV-1 (HF). Total cellular cells lysates are prepared at 24 h p.i. and subject to Western blot analysis against.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.

    IC50 & Target

    Ire1[1]

    In Vitro

    STF-083010 shows cytostatic and cytotoxic activity in a dose- and time-dependent manner. Treatment with STF-083010 shows significant antimyeloma activity in model human multiple myeloma (MM) xenografts. RPMI 8226 human MM cells grown as tumor xenografts are treated in NSG mice. Intraperitoneal injection of STF-083010 alone (day 1, day 8) significantly inhibits the growth of these tumors[1]. STF-083010 is an IRE1α-specific inhibitor. Four pancreatic cancer cell lines (Panc0403, Panc1005, BxPc3, MiaPaCa2) are treated with different combination of Bortezomib (10 or 50 nM) and STF (10 or 50 μM). The normalized isobologram analysis demonstrates synergistic activity between 10 μM STF and either 10 or 50 nM bortezomib in all four cell lines. Moreover, a higher concentration of STF (50 μM) attains synergy after addition of bortezomib either at a concentration of 10 nM when tested against BxPc3 cells, at a concentration of 50 nM against Panc1005 cells, and at either 10 or 50 nM against Panc0403 cells[2]. STF-083010 (50 μM) suppresses the growth of p53-deficient human cancer cells[3].

    In Vivo

    Treatment with STF-083010 reduces the viability of HCT116 p53-/- cells by approximately 20% compared with that of HCT116 p53-/-cells. Administration of STF-083010 to tumors induced by HCT116 p53-/- cells significantly reduces tumor volume and weight by 75% and 73% at the endpoint, respectively[3].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (315.08 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1508 mL 15.7540 mL 31.5080 mL
    5 mM 0.6302 mL 3.1508 mL 6.3016 mL
    10 mM 0.3151 mL 1.5754 mL 3.1508 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    The hIre1α protein, containing both Ire1 cytoplasmic kinase and RNase domains, is expressed and purified from baculovirus. Autophosphorylation activity is determined by the addition of 32P-γATP. Endonuclease activity is determined by the addition of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α 32P-UTP. STF083010 is incubated with recombinant hIRE1α protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers. Kinase activity and RNAse cleavage products are quantitated by polyacrylamide gel electrophoresis and 32P-γATP or 32P-UTP autoradiography, respectively[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Cell viability is determined using the MTT method. After treatment with Tunicamycin (Tm), STF-083010 (50 μM), or both, cells are incubated with MTT solution (1 mg/mL) for 2 h. Isopropanol and HCl are added to the final concentrations of 50% and 20 mM, respectively. The optical density at 570 nm is determined using a spectrophotometer using a reference wavelength of 630 nm[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    Each BALB/c nude mouse (male, 5 weeks of age) is subcutaneously inoculated in the right and left hind footpads with 5×106 HCT116 p53+/+ or HCT116 p53-/- cells. Four days later, DMSO or STF-083010 (40 mg/kg) is intraperitoneally administrated every 3 days. Tumors are measured every 5 days, and their volumes are calculated using the equation mm3=(length (mm))×(width (mm))2/2).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    317.38

    Formula

    C₁₅H₁₁NO₃S₂

    CAS No.

    307543-71-1

    SMILES

    O=S(C1=CC=CS1)(/N=C/C2=C3C=CC=CC3=CC=C2O)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >98.0%

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    Product Name:
    STF-083010
    Cat. No.:
    HY-15845
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    STF-083010

    Cat. No.: HY-15845