C646 - Moligand™, 10mM in DMSO , Inhibitor of E1A binding protein p300, CAS No.328968-36-1, Inhibitor of E1A binding protein p300

CAS: 328968-36-1 Cat. No.: C408857 Fórmula: C₂₄H₁₉N₃O₆ Peso molecular: 445.42 Número CE: 687-885-2

GRAU & PUREZA Moligand™, 10mM in DMSO

Synonyms

Benzoic acid, 4-[4-[[5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

C646 C646 is an inhibitor for histone acetyltransferase , and inhibits p300 with a K i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy .
In vitro

C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a K_i of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of these genes.

In vivo

C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord.
Cell Data

cell lines：

Concentrations：~25 μM

Incubation Time：1 to 3 hr

Powder Purity:≥97%

Especificações

Sinónimos

Benzoic acid, 4-[4-[[5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

INHIBITOR

Mecanismo de ação

Inhibitor of E1A binding protein p300

Nomes e identificadores

SMILES isoméricas

CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)/C=C\3/C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C

Peso molecular

445.42

Reaxy-Rn

20607912

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20607912&ln=

Alvos associados (humanos)

EP300 Tchem Histone acetyltransferase p300 (7 Activities)

Discover Target: EP300

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