| Molecular Weight: | 321.35 |
| Formula: | C15H15NO5S |
| Purity: | ≥98% |
| CAS#: | 321695-57-2 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | 4-((((4-methoxyphenyl)sulfonyl)oxy)imino)-2,6-dimethylcyclohexa-2,5-dienone |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
How to Use:
- In vitro: L002 was used at 5-30 µM final concentration in various in vitro assays.
- In vivo: L002 was administered through IP injection at 500 µg/100 µl twice a week for 3 weeks in xenografts models.
Reference:
- 1. 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.
