L002

• Description :

  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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CBP/p300

• CAS Number :

  [321695-57-2]