L002

Names

[ Name ]:
L002

[Synonym ]:
4-({[(4-Methoxyphenyl)sulfonyl]oxy}imino)-2,6-dimethyl-2,5-cyclohexadien-1-one
4-({[(4-Methoxyphenyl)sulfonyl]oxy}imino)-2,6-dimethylcyclohexa-2,5-dien-1-one
L002

Biological Activity

[Description]:

L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM. L002 has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases[1]. L002 blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation[2].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> STAT

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

[Target]

IC50: 1.98 uM (KAT3B); 35 µM (PCAF); 34 µM (GCN5)[1] ;STAT3; p53[2]

[References]

[1]. Rai R, et al. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013.

[2]. Sun XJ, et al. The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis. Front Oncol. 2015 May 26;5:108.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
459.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₅H₁₅NO₅S

[ Molecular Weight ]:
321.348

[ Flash Point ]:
231.9±31.5 °C

[ Exact Mass ]:
321.067108

[ LogP ]:
4.06

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.574

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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