Okadaic acid ammonium salt, a marine toxin, serves as an inhibitor of protein phosphatases (PP), displaying a higher affinity for PP2A (IC 50 =0.1-0.3 nM) alongside inhibitory effects on PP1 (IC 50 =15-50 nM), PP3 (IC 50 =3.7-4 nM), PP4 (IC 50 =0.1 nM), and PP5 (IC 50 =3.5 nM), but does not affect PP2C. By inhibiting PPs, this compound promotes protein phosphorylation and acts as a tumor promoter. Additionally, it is involved in inducing tau phosphorylation.
EIPA hydrochloride also inhibits Na+ H+-exchanger (NHE) and macropinocytosisEIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM.
CBP p300-IN-8 is a potent inhibitor of the CBP P300 family of bromodomains . CBP p300-IN-8 inhibits CBP ( IC 50 =0.01-0.1 μΜ) and BRD4 ( IC 50 =1-1000 μΜ) activity.
Thalidomide-NH-CBP p300 ligand 2 (P-007) is a PROTAC-based compound designed to degrade CBP and p300, acting as a functional antagonist (WO2020173440).
PROTAC CBP P300 Degrader-1 is an effective compound that degrades CBP P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines.