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    Resminostat (RAS2410)
    Resminostat (RAS2410)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0285
    CAS #: 864814-88-0Purity ≥98%

    Description: Resminostat (formerly RAS-2410; 4SC-201) is a potent inhibitor of classes I and II HDACs (histone deacetylases) such as HDAC1/3/6 with potential anticancer activity. It inhibits HDAC1/3/6 with IC50 values ranging from 43 to 72 nmol/L. It shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy. Resminostat is being investigated by 4SC and its Japanese partner Yakult for treating liver cancer.

    References: Br J Haematol. 2010 May;149(4):518-28.

    Related CAS #: 1187075-34-8 (HCl); 864814-88-0 (free base)

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    • 香港大学
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    Molecular Weight (MW)349.4
    FormulaC16H19N3O4S
    CAS No.864814-88-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 70 mg/mL (200.3 mM)
    Water: <1 mg/mL
    Ethanol: 70 mg/mL (200.3 mM)
    SMILES O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1
    Synonyms

    RAS2410; RAS-2410; RAS2410; RAS 2410; 4SC201; 4SC-201; 4SC 201; Resminostat

    Chemical Name: (E)-3-(1-((4-((dimethylamino)methyl)phenyl)sulfonyl)-1H-pyrrol-3-yl)-N-hydroxyacrylamide.

    InChi Key: FECGNJPYVFEKOD-VMPITWQZSA-N

    InChi Code: InChI=1S/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+

    SMILES Code: O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1


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    In Vitro

    In vitro activity: Resminostat [HCl] is acting as a potent inhibitor of recombinant HDAC 1, 3 and 6 isoenzymes with a substrate competitive binding mode. It can induce hyperacetylation of histone H4 in MM cells. Low micromolar concentrations of resminostat abrogates cell growth and strongly induces apoptosis in MM cell lines (OPM-2, NCI-H929, U266 ) as well as primary MM cells. At 1 μM, resminostat inhibits proliferation and induces G0/G1 cell cycle arrest in OPM-2, NCI-H929, U266 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21. Resminostat decreases phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Treatment with resminostat results in increased protein levels of Bim and Bax and decreases levels of Bcl-xL. Caspases 3, 8 and 9 are activated by resminostat. Furthermore, synergistic effects are observed for combinations of resminostat with melphalan and the proteasome inhibitors bortezomib and S-2209.


    Kinase Assay: Forty microliter enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat [HCl] at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10μM for HDAC6 and 25μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/ml trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the 50% inhibitory concentration (IC50) values the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) are set at 0% enzymatic activity (background fluorescence substracted). 


    Cell Assay: WST-1 assay using OPM-2, NCI-H929, RPMI-8226 and U266 cells.

    In VivoOral resminostat at 600 mg QD continuously d1−5 in a 14 day cycle is well-tolerated. Resminostat shows a favourable PK profile, with high bioavailability and low inter-pt variability. The apparent t 1/2 of oral resminostat ranged from 2.7 to 4.4 hours. The modulation of plasma biomarkers further indicates drug activity.
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    References

    Br J Haematol. 2010 May;149(4):518-28.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     


    Resminostat

    Resminostat synergizes with common and new anti‐myeloma agents. Br J Haematol. 2010 May;149(4):518-28.

     

    Resminostat

    Resminostat inhibits cell growth and induces apoptosis in MM cells. Br J Haematol. 2010 May;149(4):518-28.

    Resminostat


    Resminostat modulates expression of bcl-2 family proteins and inhibits Akt pathway signalling downstream of Akt. Br J Haematol. 2010 May;149(4):518-28.

     

     

    Resminostat

    Resminostat induces histone acetylation in myeloma cells. Br J Haematol. 2010 May;149(4):518-28.

     

     Resminostat

    Resminostat inhibits MM cell proliferation. Br J Haematol. 2010 May;149(4):518-28. Br J Haematol. 2010 May;149(4):518-28.



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