pp30

PP30 is an inhibitor of mTORC1 and mTORC2. It is selective within the PI3K family, inhibiting other PI3Ks only at high concentrations.

A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

Piflufolastat (DCFPYL) is a PET imaging agent for prostate cancer PSMA. It is a fluorinated prostate-specific membrane antigen (PSMA) preparation. Piflufolastat can be used to prepare piflufolastat F 18 (DCFPyL F-18).

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]

CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC50 values of 1.07 nM for CBP/HTRF and 5.96 nM for Myc.

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).

CBP/p300ligand 4 (Compound 4) is an orally active inhibitor of the CBP/p300 bromodomain, with an IC50 of 91.4 nM. It serves as the target protein ligand for PROTACXYD190.

CBP/p300 ligand 5 is a target protein ligand of XYD129, useful for researching acute myeloid leukemia (AML).

CBP/p300-IN-22 is a selective inhibitor of the CBP/EP300 bromodomain, with an IC50 of 4 nM. It exhibits high selectivity for BRD4(1) and reduces cytokine expression induced by TNF-α as well as subsequent immune cell recruitment by inhibiting NF-κB signaling, demonstrating anticancer properties. This compound is applicable for research into rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory diseases.

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains, inhibiting CBP with an IC50 range of 0.01-0.1 μM and BRD4 with an IC50 range of 1-1000 μM.

Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based compound engineered to degrade the proteins CBP and p300, functioning as a molecular antagonist (WO2020173440).

PROTAC CBP/P300 Degrader-1 is an effective compound that potently degrades CBP/P300, significantly reducing cell viability in various cancer cell lines.

CBP/p300 ligand 2 is the target protein ligand for PROTAC dCBP-1, a potent and selective p300/CBP degrader.

CBP/p300-IN-14, efficiently inhibits CBP/EP300 (lysine acetyltransferase) with an IC50 value of 3.3 nM.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

CBP/p300-IN-17 (compound 7) is a potent inhibitor of EP300/CBP HAT, with an IC50 of 0.18 μM for HAT EP300 and 0.69 μM for LK2 H3K27.

CBP/p300-IN-16 (compound 1) is a potent inhibitor of EP300/CBP HAT, targeting HAT EP300 with an IC50 of 0.61 μM and LK2 H3K27 with an IC50 of 2.24 μM.

CBP/p300-IN-18 (compound 8) is a potent inhibitor of EP300/CBP HAT, with an IC50 of 0.056 μM for HAT EP300 and 0.46 μM for LK2 H3K27.

CBP/p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP/p300-IN-15 can be used to study ovarian cancer.

CBP/p300-IN-19 is a potent inhibitor of p300/CBP HAT, effective against P300-HAT (IC50: 1.4 μM), CBP-HAT (IC50: 1.4 μm, 2.2 μM), PCAF (IC50: >100 μM), and Myst3 (IC50: >100 μM), demonstrating anti-tumor activity.

CBP/p300-IN-19 hydrochloride is a selective and potent inhibitor of p300/CBP HAT, with IC50 values of 1.4 μM for p300-HAT, 2.2 μM for CBP-HAT, and over 100 μM for both PCAF and Myst3, and has antitumor effects.