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Resminostat hydrochloride

CAS No. 1187075-34-8

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

产品货号. M10639 CAS No. 1187075-34-8

HDAC1/3/6 的有效抑制剂,IC50 为 43-72 nM;诱导 MM 细胞系中组蛋白 H4 的过度乙酰化和细胞凋亡 (IC50=2.5-3 uM)。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥697 有现货
10MG ¥1337 有现货
25MG ¥2633 有现货
50MG ¥4682 有现货
100MG ¥6747 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Resminostat hydrochloride
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    HDAC1/3/6 的有效抑制剂,IC50 为 43-72 nM;诱导 MM 细胞系中组蛋白 H4 的过度乙酰化和细胞凋亡 (IC50=2.5-3 uM)。
  • 产品描述
    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.
  • 体外实验
    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.
  • 体内实验
    ——
  • 同义词
    RAS2410 hydrochloride | 4SC-201 hydrochloride
  • 通路
    Cell Cycle/DNA Damage
  • 靶点
    HDAC
  • 受体
    HDAC1|HDAC3|HDAC6|HDAC8
  • 研究领域
    Cancer
  • 适应症
    Liver Cancer

化学信息

  • CAS Number
    1187075-34-8
  • 分子量
    385.8657
  • 分子式
    C16H20ClN3O4S
  • 纯度
    >98% (HPLC)
  • 溶解度
    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
  • 化学全称
    2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, hydrochloride (1:1), (2E)-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

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.
产品手册
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