Resminostat NEW

Resminostat

Modify Date: 2024-01-02 12:53:44

Resminostat structure	Common Name	Resminostat
	CAS Number	864814-88-0	Molecular Weight	349.405
	Density	1.3±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C16H19N3O4S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Purity		Quantity		Budget		Inquiry

Use of Resminostat Resminostat is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.

• Properties

• Spectrum

---

 Names

Name	(E)-3-[1-[4-[(dimethylamino)methyl]phenyl]sulfonylpyrrol-3-yl]-N-hydroxyprop-2-enamide
Synonym	More Synonyms

 Resminostat Biological Activity

Description	Resminostat is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
Related Catalog	Research Areas >> Cancer
Target	HDAC1:42.5 nM (IC50) HDAC3:50.1 nM (IC50) HDAC6:71.8 nM (IC50) HDAC8:877 nM (IC50)
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[1]. 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[2]. 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[3].
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 30 μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 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). 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 Wallac Victor2 1420 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)[1].
Cell Assay	A CCK-8 cell proliferation assay is used to investigate the antiproliferative effect of resminostat on HNSCC cells. Cells are seeded into 96-well plates at a density of 3 × 105/well. After 24 hours of growth, the cells are treated with resminostat and cisplatin, either alone or in combination and incubated for 72 hours. Untreated cells maintained in RPMI and equal concentrations of dimethylsulfoxide served as control. After 72 hours, cell proliferation is measured by CCK-8. Experiments are carried out in triplicate 3 times[2].
References	[1]. Mandl-Weber S, et al. 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]. Enzenhofer E, et al. 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]. Peng X, et al. mTOR inhibition sensitizes human hepatocellular carcinoma cells to resminostat. Biochem Biophys Res Commun. 2016 Sep 2;477(4):556-562.

 Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Molecular Formula	C16H19N3O4S
Molecular Weight	349.405
Exact Mass	349.109619
PSA	103.51000
LogP	1.69
Index of Refraction	1.600
Storage condition	-20℃

 Synonyms

Company Profile

Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.

Our Company

Our Advantage

Rich experience

Our products have been exported to many countries, including Germany, Spain, the United Kingdom, the United States, Australia, the Middle East, Asia, and more. We have received highly positive feedback from our clients and have established long-term friendly cooperative relationships with them.

Excellent quality, purity, and competitive price

Excellent quality is one of the cornerstones of our success. We welcome ordering samples for quality testing.

Safe and fast delivery

We will arrange shipment of spot products as soon as we receive payment.

Customized products are determined based on the synthesis time of different products.

Excellent pre-sales and after-sales service

Pre sales:

We are committed to providing the most favorable quotes and detailed information about our products and company.

after-sale service:

We assist buyers in customs clearance by providing necessary documents and information.

If there is any dispute over product quality, we are committed to providing the best solution.

• Packaging: 

1kg/bag, 25kg/drum, 50kg/drum, 180kg/drum, 200kg/drum, 1T/bag/drum, standard export packaging or packaging required by customers

• Shipping

• Delivery:

Within 7 days after receiving your payment

Contact information

For more details, pls contact us freely.

Contact name: Tina

Email address: Tina@fdachem.com

Mob: 86 13213167925

WhatsApp/Skype/Wechat/LINE: 86 15225627621