Resminostat hydrochloride

CAS No. 1187075-34-8

Resminostat hydrochloride( RAS2410 hydrochloride | 4SC-201 hydrochloride )

Catalog No. M10639 CAS No. 1187075-34-8

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).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 77 Get Quote
10MG 149 Get Quote
25MG 293 Get Quote
50MG 520 Get Quote
100MG 750 Get Quote
200MG Get Quote Get Quote
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Biological Information

  • Product Name
    Resminostat hydrochloride
  • Note
    Research use only, not for human use.
  • Brief 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).
  • 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 hydrochloride (Resminostat [HCl], 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 Vitro
    Resminostat hydrochloride (Resminostat [HCl], 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 hydrochloride | 4SC-201 hydrochloride
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    HDAC
  • Recptor
    HDAC1|HDAC3|HDAC6|HDAC8
  • Research Area
    Cancer
  • Indication
    Liver Cancer

Chemical Information

  • CAS Number
    1187075-34-8
  • Formula Weight
    385.8657
  • Molecular Formula
    C16H20ClN3O4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 50 mg/mL
  • SMILES
    O=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1.[H]Cl
  • Chemical Name
    2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, hydrochloride (1:1), (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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