Epacadostat (INCB024360) - Moligand™, 10mM in DMSO , Indoleamine 2,3-dioxygenase inhibitor, CAS No.1204669-58-8, Indoleamine 2,3-dioxygenase inhibitor

CAS: 1204669-58-8 Cat. No.: E409041 Molecular Weight: 438.23 EC Number: 815-121-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

[C(Z)]-4-[[2-[(aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Epacadostat (INCB024360) Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
In vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells.

In vivo

INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

[C(Z)]-4-[[2-[(aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1, 2, 5-oxadiazole-3-carboximidamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Epacadostat (INCB024360) is a potent and selective indoleamine 2, 3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2, 3-dioxygenase (TDO).

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Indoleamine 2, 3-dioxygenase inhibitor

Names and Identifiers

• Isomeric SMILES: C1=CC(=C(C=C1N=C(C2=NON=C2NCCNS(=O)(=O)N)NO)Br)F
• Molecular Weight: 438.23
• Reaxy-Rn: 30500508
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30500508&ln=

Associated Targets(Human)

IDO2 Tchem Indoleamine 2,3-dioxygenase 2 (1 Activities)

Discover Target: IDO2

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

TDO2 Tchem Tryptophan 2,3-dioxygenase (3 Activities)

Discover Target: TDO2

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

IDO1 Tchem Indoleamine 2,3-dioxygenase 1 (58 Activities)

Discover Target: IDO1

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