pp 3

PP 3 is a Negative control for the Src kinase inhibitor PP 2

Okadaic acid is a potent polyether marine toxin that primarily accumulates in the digestive glands of marine mollusks. It is a highly effective and selective inhibitor of protein phosphatases (PPs). By inhibiting these phosphatases, okadaic acid increases the phosphorylation levels of various proteins, acts as a tumor promoter, and induces tau protein phosphorylation. It can be used to establish models of Alzheimer’s disease and skin cancer.

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

3BrB-PP1 is an ATP-competitive analog that exhibits specific inhibitory activity towards protein kinase, particularly effective against protein kinases with mutations in the ATP-binding pocket, such as the Thr97 mutation within Sty1's ATP-binding pocket.

3-IN-PP1, a potent protein kinase D (PKD) inhibitor, exhibits pan-PKD inhibitory activity with IC50 values of 108 nM for PKD1, 94 nM for PKD2, and 108 nM for PKD3. Additionally, it serves as a broad-spectrum anticancer agent by inhibiting the growth of various tumor cells. 3-IN-PP1 is utilized in cancer research [1].

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]

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp/Carbonic anhydrase-IN-2 induced apoptosis.Enpp/Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.

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.

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-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).

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

ENPP3 Inhibitor 1 is a selective inhibitor of ENPP3, exhibiting an IC50 value of 0.15 µM, compared to an IC50 of 41.4 µM for ENPP1. It demonstrates antitumor effects against breast and cervical cancers.

NPP3-IN-1 (Compound 3e) is an inhibitor of phosphodiesterase/pyrophosphatase-3 (NPP3), exhibiting IC50 values of 0.24 μM for NPP3 and 1.37 μM for NPP1.

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.

5HPP-33 is an microtubule-stabilizer with the properties of antiproliferative and antimitotic.

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