Name: Resminostat
Brand: Selleck Chemicals
SKU: S2693
Availability: InStock
Rating: 5 (8 reviews)

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Batch: S269301 DMSO]70 mg/mL]false]Ethanol]70 mg/mL]false]Water]Insoluble]false Purity: 99.04%

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COA
NMR
HPLC
SDS
Datasheet

99.04

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Inhibitors	Entinostat (MS-275) RGFP966 Tubastatin A Tubastatin A HCl Fimepinostat (CUDC-907) Trichostatin A (TSA) Mocetinostat (MGCD0103) Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) Dihydrochloride MC1568

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (200.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 70 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (8.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.875mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 17.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Average weight of animals: g

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	349.4	Formula	C₁₆H₁₉N₃O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	864814-88-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RAS2410			Smiles	CN(C)CC1=CC=C(C=C1)S(=O)(=O)N2C=CC(=C2)C=CC(=O)NO

Mechanism of Action

Targets/IC₅₀/Ki	HDAC1 42.5 nM HDAC3 50.1 nM HDAC6 71.8 nM
In vitro	Resminostat [HCl] is acting as a potent inhibitor of recombinant HDAC 1, 3 and 6 isoenzymes with a substrate competitive binding mode. It can induce hyperacetylation of histone H4 in MM cells. Low micromolar concentrations of this compound abrogates cell growth and strongly induces apoptosis in MM cell lines (OPM-2, NCI-H929, U266 ) as well as primary MM cells. At 1 μM, this chemical inhibits proliferation and induces G0/G1 cell cycle arrest in OPM-2, NCI-H929, U266 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21. This compound decreases phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Treatment with this agent results in increased protein levels of Bim and Bax and decreases levels of Bcl-xL. Caspases 3, 8 and 9 are activated by it. Furthermore, synergistic effects are observed for combinations of this compound with melphalan and the proteasome inhibitors bortezomib and S-2209.
Kinase Assay	Enzymatic HDAC activity assays
Kinase Assay	Forty microliter 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 μL enzyme buffer and 1 μL resminostat [HCl] at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10μM for HDAC6 and 25μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/ml trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the 50% inhibitory concentration (IC50) values the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) are set at 0% enzymatic activity (background fluorescence substracted).
In vivo	Oral resminostat at 600 mg QD continuously d1−5 in a 14 day cycle is well-tolerated. This compound shows a favourable PK profile, with high bioavailability and low inter-pt variability. The apparent t _1/2 of this compound ranged from 2.7 to 4.4 hours. The modulation of plasma biomarkers further indicates drug activity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20201941/ [2] http://www.ejcancersupplements.com/article/S1359-6349%2808%2972327-9

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04955340	Completed	Cutaneous T Cell Lymphoma\|Mycosis Fungoides\|Sezary Syndrome	4SC AG	October 12 2021	Phase 1
NCT01277406	Completed	Advanced Colorectal Carcinoma	4SC AG	January 2011	Phase 1\|Phase 2
NCT01037478	Completed	Hodgkin''s Lymphoma	4SC AG	December 2009	Phase 2

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Resminostat HDAC inhibitor

Chemical Structure

Molecular Weight: 349.4