PF CBP1 is a selective CBP/p300 bromodomain inhibitor (IC50 values are 0.13 and 18.1 μM, respectively). Exhibits >100-fold selectivity for CBP over BRD4. Also exhibits selectivity over a panel of other bromodomains. Reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. Also downregulates RGS4 expression in primary cortical neurons in vitro.
Biochem Pharmacol. 2022 Oct 31;206:115334.
MCP-1 facilitates VEGF production by removing miR-374b-5p blocking of VEGF mRNA translation
PF CBP1 purchased from AbMole
| Molecular Weight | 488.62 |
| Formula | C29H36N4O3 |
| CAS Number | 1962928-21-7 |
| Solubility (25°C) | DMSO 48.86 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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