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Resminostat hydrochloride

In stock
Catalog No.
A3755
HDAC inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$291.00
In stock
10mg
$265.00
In stock
50mg
$827.00
In stock
100mg
$1,326.00
In stock

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Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6 [1].

As an inhibitor of HDACs, resminostat also inhibits HDAC8 with a weak activity (IC50=877nM). 5μM resminostat induces the acetylation of histone H4 in U266 myeloma cells. 10μM resminostat completely suppresses the cell growth in human myeloma cell lines, such as OPM-2, RPMI-8226 and U266. This inhibition is proved to be caused by the induction of apoptosis. In primary myeloma cells, resminostat also induces apoptosis of cells. Besides that, resminostat is proved to downregulate the expression of cell cycle proteins, including phosphorylated Rb, cdc25a, cyclin D1, Cdk4 and p53. In addition, resminostat is reported to be well tolerated, have no unexpected toxicities and do not cause clinically significant myelosuppression in the first-human study [1, 2].

References:
[1] Mandl-Weber S, Meinel FG, Jankowsky R, Oduncu F, Schmidmaier R, Baumann P. 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] Brunetto AT, Ang JE, Lal R, Olmos D, Molife LR, Kristeleit R, Parker A, Casamayor I, Olaleye M, Mais A, Hauns B, Strobel V, Hentsch B, de Bono JS. First-in-human, pharmacokinetic and pharmacodynamic phase I study of Resminostat, an oral histone deacetylase inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2013 Oct 1;19(19):5494-504.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt385.87
Cas No.1187075-34-8
FormulaC16H20ClN3O4S
SynonymsRAS2410 hydrochloride;4SC-201 hydrochloride;RAS 2410 hydrochloride;RAS-2410 hydrochloride
SolubilitySoluble in DMSO
Chemical Name(Z)-3-(1-((4-((dimethylamino)methyl)phenyl)sulfonyl)-1H-pyrrol-3-yl)-N-hydroxyacrylamide hydrochloride
SDFDownload SDF
Canonical SMILESCN(C)CC1=CC=C(S(=O)(N2C=C(/C=C\C(NO)=O)C=C2)=O)C=C1.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Resminostat hydrochloride