L002

L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM[1]. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation[2]. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment[3].

Product Specifications

CAS Number

[321695-57-2]

UNSPSC

12352005

Target

Histone Acetyltransferase; STAT

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/l002.html

Purity

99.44

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

O=C1C(C)=C/C(C=C1C)=N\OS(=O)(C2=CC=C(OC)C=C2)=O

Molecular Formula

C15H15NO5S

Molecular Weight

321.35

References & Citations

[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.|[3]Rai R, et al. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis.J Cell Mol Med. 2019 Apr;23 (4) :3026-3031.