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 |
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10MG | 149 | Get Quote |
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25MG | 293 | Get Quote |
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50MG | 520 | Get Quote |
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100MG | 750 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameResminostat hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionA 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).
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DescriptionA 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.
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In VitroResminostat 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.
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In Vivo——
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SynonymsRAS2410 hydrochloride | 4SC-201 hydrochloride
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PathwayCell Cycle/DNA Damage
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TargetHDAC
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RecptorHDAC1|HDAC3|HDAC6|HDAC8
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Research AreaCancer
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IndicationLiver Cancer
Chemical Information
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CAS Number1187075-34-8
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Formula Weight385.8657
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Molecular FormulaC16H20ClN3O4S
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 50 mg/mL
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SMILESO=C(NO)/C=C/C1=CN(S(=O)(C2=CC=C(CN(C)C)C=C2)=O)C=C1.[H]Cl
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Chemical Name2-Propenamide, 3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-, hydrochloride (1:1), (2E)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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