GSK 4027 - Moligand™, 10mM in DMSO , CAS No.2079896-25-4

CAS: 2079896-25-4 Cat. No.: G655167 Fórmula: C₁₇H₂₁BrN₄O Peso molecular: 377.28 PubChem CID: 126961735

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

GSK 4027 is a chemical probe for the PCAF / GCN5 bromodomain with an pIC 50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

In Vitro

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC 50 s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pK i of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with K i of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC 50 7.2 (IC 50 60 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:pIC50: 7.4±0.11 (PCAF)

Specifications

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

GSK 4027 is a chemical probe for the PCAF / GCN5 bromodomain with an pIC 50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CN1C[C@H](C[C@H](C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3
• PubChem CID: 126961735
• Términos de entrada MeSH: 4-bromo-2-methyl-5-((1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one;GSK4027;GSK4028
• Peso molecular: 377.28

Objetivos asociados (humanos)

KAT2A Tchem Histone acetyltransferase KAT2A (2 Activities)

Discover Target: KAT2A

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

KAT2B Tchem Histone acetyltransferase KAT2B (5 Activities)

Discover Target: KAT2B

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

BRPF3 Tchem Bromodomain and PHD finger-containing protein 3 (1 Activities)

Discover Target: BRPF3

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