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 Peso molecular: 445.42 Número EC: 687-885-2

GRADE & PURITY 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

Descripción general

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%

Specifications

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]-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y 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.

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

Mecanismo de acción

Inhibitor of E1A binding protein p300

Nombres e identificadores

• Isómeros SMILES: 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=

Objetivos asociados (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)

Referencias

1. Guo Xiaoyu, Zhong Jinjing, Qian Jingyu, Pan Xiuyi, Zhang Xinyue, Chen Xueqin, Zeng Hao, Chen Ni, Nie Ling, Yu Ting, Zhou Qiao.  (2025)  tRF-21LeuTAA Promotes Oxidative Stress by Altering Glutathione Metabolic Enzymes to Support Prostate Cancer Progression.  CANCER RESEARCH,      [PMID:40882020] [10.1158/0008-5472.CAN-25-0273]

2. Yu Cao, Yang Zhao, Tan Deng, Qigang Zhou, Gang Hu, Zhuang-Li Hu, Yan-Yi Jiang, Xiao-Han Yang, Fang Wang, Peng-Fei Wu, Jian-Guo Chen.  (2025)  Hepatic acetyl-CoA metabolism modulates neuroinflammation and depression susceptibility via acetate.  Cell Metabolism,      [PMID:40992374] [10.1016/j.cmet.2025.08.010]

3. Xiaoqi Wang, Shuang Liu, Di Su, Jiayu Sui, Xiangyu Yan, Jia Yang, Ziqi Zheng, Penghe Wang, Weijun Song, Zexi Jin, Mingyan E, Maomao Zhang, Bo Yu.  (2025)  Alpha-lipoic acid attenuates cardiac inflammation of CVB3 induced viral myocarditis via neutrophil-derived YM-1.  BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE,      [PMID:40925469] [10.1016/j.bbadis.2025.168034]

4. Ming-Yue Bao, Xiu-Qing Li, Qing-Qing Sun, Yan He, Yu-Jing Yin, Si-Han Li, Ruo-Yan Du, Gai-Xin Ma, Chen-Yu Feng, Bing Han, Rui Jia, Xuan Wang, Li-Bin Wang, Ya-Ping Yan, Xing Li, Yuan Zhang.  (2026)  Oligodendrocyte-encoded lactate dehydrogenase A couples glycolysis to remyelination via protein lactylation.  NEURON,      [PMID:41844160] [10.1016/j.neuron.2026.02.032]