Droxinostat - Moligand™, 10mM in DMSO , Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6;Inhibitor of histone deacetylase 8, CAS No.99873-43-5, Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6;Inhibitor of histone deacetylase 8

CAS: 99873-43-5 Cat. No.: D409135 Peso molecular: 243.69 Número EC: 662-725-4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NS 41080 | 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Droxinostat (NS 41080) is a selective inhibitor ofHDAC, mostly for HDACs 6 and 8 withIC50of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
In vitro

Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). In PPC-1 cells cultured in suspension but not adherent conditions, Droxinostat (20 μM–60 μM) sensitizes cells to anoikis by initially activating caspase 8 with subsequent activation of the mitochondrial pathway. Similarly, Droxinostat also sensitizes other cancer cell lines including PC-3, DU-145, T47D, and OVCAR-3, but not LNCaP or MB-MDA-468, to anoikis or CH-11-induced apoptosis. However, the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIP_L and c-FLIP_S expression, reducing cell survival, and inducing apoptosis.

In vivo

In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.
Cell Data

cell lines：MEFs

Concentrations：0–100 μM, dissolved in DMSO (final concentration of DMSO is 0.5%)

Incubation Time：24 hours

Powder Purity:≥96%

Specifications

Sinónimos

NS 41080 | 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Droxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of histone deacetylase 3;Inhibitor of histone deacetylase 6;Inhibitor of histone deacetylase 8

Nombres e identificadores

• Isómeros SMILES: CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO
• WGK Alemania: 3
• Peso molecular: 243.69
• Reaxy-Rn: 11721332
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11721332&ln=

Objetivos asociados (humanos)

HDAC6 Tclin Histone deacetylase 6 (1 Activities)

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC8 Tclin Histone deacetylase 8 (1 Activities)

Discover Target: HDAC8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC3 Tclin Histone deacetylase 3 (1 Activities)

Discover Target: HDAC3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro Water: 39 mg/mL (198.86 mM); DMSO: Insoluble