IKK-16 (IKK Inhibitor VII) - 10mM in DMSO , CAS No.873225-46-8

CAS: 873225-46-8 Cat. No.: I408739 Peso molecular: 483.63 Número EC: 809-503-7

GRADE & PURITY 10mM in DMSO

Synonyms

Methanone, [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor forIKK-2,IKK complexandIKK-1withIC50of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in
In vitro

IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker.

In vivo

IKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

Methanone, [4-[(4-benzo[b]thien-2-yl-2-pyrimidinyl)amino]phenyl][4-(1-pyrrolidinyl)-1-piperidinyl]-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activ

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.

Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: C1CCN(C1)C2CCN(CC2)C(=O)C3=CC=C(C=C3)NC4=NC=CC(=N4)C5=CC6=CC=CC=C6S5
• Peso molecular: 483.63
• Reaxy-Rn: 10307514
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10307514&ln=

Objetivos asociados (humanos)

PRKCZ Tchem Protein kinase C zeta type (1 Activities)

Discover Target: PRKCZ

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

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 38 mg/mL (197.74 mM)