L002 (NSC764414) is a novel selective, cell permeable and reversible inhibitor of p300 histone acetyl transferase (IC50 ~1.98 µM). It has no activity in histone methyltransferases tested, including DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2 etc. L002 was shown to occupy Ac-CoA binding pocket of p300, and is less potent to CBP, PCAF, GCN5 and GNAT. It suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. L002 can suppress tumor growth and histone acetylation in a mouse MDA-MB-468 xenograft model.
CAS Number: 321695-57-2
Molecular Weight: 321.35
Chemical Name: 4-((((4-methoxyphenyl)sulfonyl)oxy)imino)-2,6-dimethylcyclohexa-2,5-dienone
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
L002 was used at 5-30 µM final concentration in various in vitro assays.
L002 was administered through IP injection at 500 µg/100 µl twice a week for 3 weeks in xenografts models.
- Yang H, et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. (2013) Mol Cancer Ther. 12(5):610-20.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.