Resminostat

CAS No. 864814-88-0

Resminostat( RAS2410 | 4SC-201 | RAS 2410 | RAS-2410 )

Catalog No. M16273 CAS No. 864814-88-0

A potent inhibitor of HDAC1/3/6 with IC50s of 43-72 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Resminostat
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent inhibitor of HDAC1/3/6 with IC50s of 43-72 nM.
  • Description
    A potent inhibitor of HDAC1/3/6 with IC50s of 43-72 nM; induces hyperacetylation of histone H4 and apoptosis in MM cell lines (IC50=2.5-3 uM); decreases levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21; downregulates phosphorylation of 4E-BP1 and p70S6k.Liver Cancer Phase 2 Clinical.
  • In Vitro
    Resminostat (RAS2410; 4SC-201; 5 μM) induces histone acetylation in myeloma cells. Resminostat hydrochloride displays a substrate competitive binding mode with a mean Ki value of 27 nM. Resminostat hydrochloride (5 μM) induces histone hyperacetylation in myeloma cells. Resminostat inhibits cell growth, induces apoptosis and inhibits MM cell proliferation. Resminostat (5 μM) also modulates expression of bcl-2 family proteins and inhibits Akt pathway signalling downstream of Akt. Resminostat exerts synergistic activity against myeloma cells when combined with common and new anti-myeloma agents. Resminostat inhibits cell growth in head and neck squamous cell carcinoma cell lines, with IC50s ranging from 0.775 μM to 1.572 μM (IC50 for SCC25: 0.775 μM; CAL27: 1.572 μM; and FaDu: 0.899 μM). Resminostat (1.25 and 2.5 μM) has a synergistic effect with irradiation on HNSCC cell lines. Resminostat in combination with cisplatin induces a downregulation of survivin. However, Resminostat shows no effect on Mcl-1 and p-AKT expression.Resminostat reduces viability of HCC cells with the co-treatment of AZD-2014, with IC50s ranging from 0.89 ± 0.12 μM to 0.07 ± 0.01 μM.
  • In Vivo
    ——
  • Synonyms
    RAS2410 | 4SC-201 | RAS 2410 | RAS-2410
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    HDAC
  • Recptor
    HDAC1| HDAC3| HDAC6
  • Research Area
    Cancer
  • Indication
    Liver Cancer

Chemical Information

  • CAS Number
    864814-88-0
  • Formula Weight
    349.4048
  • Molecular Formula
    C16H19N3O4S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1
  • Chemical Name
    2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, (2E)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Mandl-Weber S, et al. Br J Haematol. 2010 May;149(4):518-28. 2. Fu M, et al. Biochem Biophys Res Commun. 2016 Sep 2;477(4):527-33. 3. Enzenhofer E, et al. Head Neck. 2017 May;39(5):900-907.
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