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Resminostat

Resminostat structure

CAS No:
864814-88-0
Formula:
C16H19N3O4S
Chemical Name:
Resminostat
Synonyms:
2-Propenamide,3-[1-[[4-[(dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-,(2E)-;(2E)-3-[1-[[4-[(Dimethylamino)methyl]phenyl]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxy-2-propenamide;(E)-3-[1-[[4-[(Dimethylamino)methyl]benzene]sulfonyl]-1H-pyrrol-3-yl]-N-hydroxyacrylamide;Resminostat;4SC 201
Categories:
Biochemical Engineering > Inhibitors

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.

Resminostat has been used in trials studying the treatment of Sezary Syndrome, Mycosis fungoides, Hodgkin's Lymphoma, Hepatocellular Carcinoma, and Lymphoma, T-Cell, Cutaneous, among others.|Resminostat is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, inhibition of the transcription of tumor suppressor genes, inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.

Resminostat Basic Attributes

Molecular Weight：

349.40476

Exact Mass：

349.40

UNII：

1578EUB98L

DSSTox ID：

DTXSID50235587

NCI Thesaurus Code：

C84856

Characteristics

PSA：

100

XLogP3：

1.69

Density：

1.3±0.1 g/cm3

Refractive Index：

1.600

Drug Information

Drug Indication：

Treatment of Cutaneous T-Cell Lymphoma

MeSH Entry Terms：

RAS 2410

Resminostat Use and Manufacturing

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:349.4
XLogP3:0.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:6
Exact Mass:349.10962727
Monoisotopic Mass:349.10962727
Topological Polar Surface Area:100
Heavy Atom Count:24
Complexity:548
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Resminostat(RAS2410)

CAS No.: 864814-88-0

Content: 0.98%

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