| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S8625 | GNE-049 | GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. |
|
|
| S1161 | Histone Acetyltransferase Inhibitor II |
Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells. |
|
|
| S2966 | TTK21 | TTK21 is an activator of the histone acetyltransferases CBP/p300. It activates CBP/p300 histone acetyltransferase activity in a concentration-dependent manner with a maximal effect at a concentration of 275 µM. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different brain parts when conjugated to glucose-based carbon nanosphere (CSP). |
|
|
| S6876 | CPI-1612 | CPI-1612 is a highly potent, orally active inhibitor of EP300/CBP histone acetyltransferase (HAT). It displays an IC50 of 8.0 nM for EP300 HAT. CPI-1612 suppresses H3K27 acetylation in vivo and exhibits efficacy in JEKO-1 mantle cell lymphoma xenograft at a low dose. CPI-1612 displays anticancer activity. | ||
| S7152 | C646 | C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
|
|
| S9648 | NEO2734 (EP31670) | NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
|
|
| S0022 | YF-2 | YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, this compound has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. It also increases p300 activity. |
|
|
| S3984 | Nordihydroguaiaretic acid (NDGA) | Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. |
|