Resminostat (RAS2410)

Alias: RAS2410; RAS-2410; RAS2410; RAS 2410; 4SC201; 4SC-201; 4SC 201; Resminostat
Cat No.:V0285 Purity: ≥98%
Resminostat (formerly RAS-2410; 4SC-201) is a potent inhibitor of classes I and II HDACs (histone deacetylases) such as HDAC1/3/6 with potential anticancer activity.
Resminostat (RAS2410) Chemical Structure CAS No.: 864814-88-0
Product category: HDAC
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Resminostat (formerly RAS-2410; 4SC-201) is a potent inhibitor of classes I and II HDACs (histone deacetylases) such as HDAC1/3/6 with potential anticancer activity. With IC50 values between 43 and 72 nmol/L, it inhibits HDAC1/3/6. Both in vivo and in vitro antitumor efficaciousness are strong points of this substance. 4SC is exploring the use of resminostat as a liver cancer treatment partner with Yakult in Japan.

Biological Activity I Assay Protocols (From Reference)
Targets
HDAC1 ( IC50 = 42.5 nM ); HDAC3 ( IC50 = 50.1 nM ); HDAC6 ( IC50 = 71.8 nM ); HDAC8 ( IC50 = 877 nM )
ln Vitro

Resminostat (RAS2410; 4SC-201; 5 μM) causes histone acetylation. in myeloma cells. Resminostat hydrochloride has a mean Ki value of 27 nM, indicating a substrate competitive binding mode. Histone hyperacetylation is induced in myeloma cells by 5 μM of resminostat hydrochloride. Resminostat suppresses the growth of cells, triggers apoptosis, and reduces the number of MM cells. Resminostat (5 μM) also affects the expression of proteins in the bcl-2 family and prevents signaling through the Akt pathway that occurs after Akt. Combining resminostat with both established and novel anti-myeloma agents has a synergistic effect on myeloma cells[1].
Resminostat shows 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) in head and neck squamous cell carcinoma cell lines, indicating that it inhibits cell growth. HNSCC cell lines respond well to both irradiation and resminostat (1.25 and 2.5 μM). One can downregulate survivin by combining resminostat with cisplatin. On Mcl-1 and p-AKT expression, however, Resminostat has no effect[2].
Resminostat decreases HCC cell viability when combined with AZD-2014; IC50s range from 0.89 ± 0.12 μM to 0.07 ± 0.01 μM[3].

ln Vivo
Resminostat taken orally at 600 mg QD every day for 1–5 days in a 14-day cycle is well tolerated. With low inter-pt variability and high bioavailability, resminostat exhibits a favorable pharmacokinetic profile. Oral resminostat's apparent t1/2 varied from 2.7 to 4.4 hours. Additional evidence of medication activity is the modulation of plasma biomarkers.
Enzyme Assay
A 96-well microtitre plate is filled with 40 microliters of enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6, or 8 activity, 29 microliters of enzyme buffer, and 1 microliter of resminostat [HCl] at varying concentrations. The reaction is initiated by adding 30 microliters of substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations of 6 μM for HDAC1, 10 μM for HDAC6, and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). The reaction is stopped by adding 25 μL of stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin, and 2 μM trichostatin A [TSA]) after the enzymes have been incubated for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C. The quantification of AMC produced by tryptic cleavage of the deacetylated peptide is done using a Wallac Victor2 1420 multilabel counter (extinction 355 nm, emission 460 nm) following an additional 40 minutes of room temperature incubation. The fluorescence in wells without test compound (1% DMSO, negative control) is set to 100% enzymatic activity for the calculation of the 50% inhibitory concentration (IC50) values, while the fluorescence in wells with 2 μM TSA (positive control) is set to 0% enzymatic activity (background fluorescence substracted)[1].
Cell Assay
The antiproliferative effect of resminostat on HNSCC cells is examined using a CCK-8 cell proliferation assay. Three × 105 cells per well are seeded into 96-well plates. Following a 24-hour growth period, the cells undergo treatment with resminostat and cisplatin, either separately or in conjunction, and are then incubated for a full 72 hours. Equal amounts of dimethylsulfoxide were used as a control group along with untreated cells that were kept in RPMI. CCK-8 is used to measure the proliferation of cells after 72 hours. Three times, each experiment is conducted in triplicate[2].
Animal Protocol


References

[1]. The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. Br J Haematol. 2010 May;149(4):518-28.

[2]. Effect of the histone deacetylase inhibitor resminostat on head and neck squamous cell carcinoma cell lines. Head Neck. 2017 May;39(5):900-907.

[3]. mTOR inhibition sensitizes human hepatocellular carcinoma cells to resminostat. Biochem Biophys Res Commun. 2016 Sep 2;477(4):556-562.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H19N3O4S
Molecular Weight
349.4
Exact Mass
349.11
Elemental Analysis
C, 55.00; H, 5.48; N, 12.03; O, 18.32; S, 9.18
CAS #
864814-88-0
Appearance
Solid powder
SMILES
CN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(=C2)/C=C/C(=O)NO
InChi Key
FECGNJPYVFEKOD-VMPITWQZSA-N
InChi Code
InChI=1S/C16H19N3O4S/c1-18(2)11-13-3-6-15(7-4-13)24(22,23)19-10-9-14(12-19)5-8-16(20)17-21/h3-10,12,21H,11H2,1-2H3,(H,17,20)/b8-5+
Chemical Name
(E)-3-[1-[4-[(dimethylamino)methyl]phenyl]sulfonylpyrrol-3-yl]-N-hydroxyprop-2-enamide
Synonyms
RAS2410; RAS-2410; RAS2410; RAS 2410; 4SC201; 4SC-201; 4SC 201; Resminostat
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~70 mg/mL (~200.3 mM)
Water: <1 mg/mL
Ethanol: ~70 mg/mL (~200.3 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8620 mL 14.3102 mL 28.6205 mL
5 mM 0.5724 mL 2.8620 mL 5.7241 mL
10 mM 0.2862 mL 1.4310 mL 2.8620 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02953301 Active
Recruiting
Drug: resminostat
Drug: Placebo
Mycosis Fungoides
Sezary Syndrome
4SC AG November 2016 Phase 2
NCT04525729 Recruiting Drug: RAS 2410
Drug: Rituximab
IgA Nephropathy CHENNAN July 1, 2020 Phase 4
NCT04955340 Completed Drug: [14C]-resminostat Mycosis Fungoides
Sezary Syndrome
4SC AG October 12, 2021 Phase 1
NCT01037478 Completed Drug: Resminostat
(4SC-201)
Hodgkin's Lymphoma 4SC AG December 2009 Phase 2
NCT02400788 Completed Drug: Resminostat
Drug: Sorafenib
Hepatocellular Carcinoma Yakult Honsha Co., LTD April 2013 Phase 1
Phase 2
Biological Data

  • Resminostat

    Resminostat synergizes with common and new anti‐myeloma agents.Br J Haematol. 2010 May;149(4):518-28.

  • Resminostat

    Resminostat inhibits cell growth and induces apoptosis in MM cells.Br J Haematol. 2010 May;149(4):518-28.

  • Resminostat


    Resminostat modulates expression of bcl-2 family proteins and inhibits Akt pathway signalling downstream of Akt.Br J Haematol.2010 May;149(4):518-28.

  • Resminostat

    Resminostat induces histone acetylation in myeloma cells.Br J Haematol. 2010 May;149(4):518-28.

  • Resminostat

    Resminostat inhibits MM cell proliferation. Br J Haematol. 2010 May;149(4):518-28.Br J Haematol. 2010 May;149(4):518-28.

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