Resminostat

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

HDAC1/3/6 的有效抑制剂，IC50 为 43-72 nM。

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.

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.

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RAS2410 | 4SC-201 | RAS 2410 | RAS-2410

Cell Cycle/DNA Damage

HDAC

HDAC1| HDAC3| HDAC6

Cancer

Liver Cancer

864814-88-0

349.4048

C16H19N3O4S

>98% (HPLC)

10 mM in DMSO

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

2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years