| Name | L002 |
| Description | L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis. |
| In vitro | L002 also has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 μM, respectively) and is specific for p300 over a panel of deacetylases, additional acetyltransferases, and methyltransferases. |
| In vivo | L002 reverses hypertension‐induced cardiac hypertrophy and fibrosis by treatment of mice after inducing hypertension for two weeks significantly.It also reduces the levels of perivascular and interstitial collagen in the myocardium compared to non-treated hypertensive mice. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.22 mM), Sonication is recommended.
DMSO : 60 mg/mL (186.71 mM), Sonication is recommended.
|
| Keywords | STAT | PCAF | p300 | L-002 | L002 | L 002 | KAT3B | Inhibitor | inhibit | HistoneAcetyltransferase | Histone Acetyltransferase | histone | HATs | HAT | GCN5 | fibrosis | cardiac | acetylation |
| Inhibitors Related | Flubendazole | HODHBt | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | Acetaminophen | Nifuroxazide | Balsalazide disodium dihydrate | Manganese chloride (tetrahydrate) | Curcumin | Niclosamide | N4-Acetylcytidine | Naphthol AS-E | Niclosamide olamine |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Hematonosis Compound Library | JAK-STAT Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Anti-Cardiovascular Disease Compound Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Liver Cancer Compound Library | Anti-Hypertension Compound Library |
United States
