pp-2

PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.

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.

CLPP-2068 has oral activity and is an activator of human casein hydrolase P (HsClpP) (EC50=50.4 nM). CLPP-2068 exhibits anti proliferative effects (IC50=5.2 nM) in OCI-LY10 cells, and can also reduce mitochondrial membrane potential, increase mitochondrial ROS levels, and induce mitochondrial dysfunction. CLPP-2068 blocks the cell cycle in G1 phase and induces apoptosis in OCI-LY10 cells. CLPP-2068 exhibits anti-tumor activity in a mouse xenograft model.

BPP-2 is a GHSR ligand containing the element F. By labeling BPP-2 with the isotope 18F, a PET probe targeting GHSR can be produced. The binding affinity (Ki) of 18F-BPP-2 for GHSR is 274 nM.

SLUPP-225 is an efflux pump inhibitor (EPI) by interacting with the membrane fusion protein AcrA, a critical component of the AcrAB-TolC efflux pump in Escherichia coli.

HPP-2 is a novel phosphodiesterase 10A (PDE10A) inhibitor used to treat schizophrenia.

DPP-21 is an inhibitor of microtubule protein polymerization (IC50: 2.4 μM). It exhibits antiproliferative activity against various cancer cell lines, with IC50 values of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23), and 9.37 nM (HepG2). DPP-21 induces cell cycle arrest at the G2/M phase of mitosis and subsequently triggers apoptosis in tumor cells by decreasing Bcl-2 while increasing pro-apoptotic protein Bax levels.

Iptacopan (LNP023) is an inhibitor with high affinity to factor B, with a KD value of 7.9 nM and an IC50 value of 10 nM.

DT-061, an orally bioavailable protein phosphatase 2A (PP2A) activator, may be used in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride may cause sensitization. Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride promotes apoptosis in HepG2 (IC50= 62 μM) and SK-Hep1 (IC50= 151 μM) cells and inhibits protein phosphatase 2A.

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.

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).

PP2 Analog is an analog of PP2. It also acts as a protein trafficking modulator.

Sanguinarine chloride (Pseudochelerythrine chloride), a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).

SMAP-2 is an orally bioavailable activator of phosphatase 2A (PP2A) which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. It inhibits the growth of KRAS-mutant lung cancers .

Calyculin A ((-)-Calyculin A), a toxicant in the Japanese marine sponge CDiscodermia calyxC, is a selective and potent inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), inducing hyperactivation of cryopreserved bovine spermatozoa and inhibiting radiation-induced gammaH2AX DNA repair disease in human lymphocytes. gammaH2AX DNA repair foci in human lymphocytes.

Voclosporin (ISAtx-247) is a novel, orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant used for treating lupus nephritis.

(Rac)-LB-100, a novel Protein Phosphatase 2A (PP2A) inhibitor, sensitizes malignant meningioma cells to the therapeutic effects of radiation

Fenvalerate (Evercide 2362) is a inhibitor of protein phosphatase 2B (calcineurin), a synthetic pyrethroid insecticide, and inhibits PP2B-Aα.High doses of Fenvalerate impair cognitive and behavioral development.Fenvalerate induces, through the Fas/FasL signaling pathway, the induction of Fenvalerate induces germ cell apoptosis in mouse testis through the Fas/FasL signaling pathway.

Pirimiphos-ethyl is used as an organophosphorus pesticide.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

N-Stearoylsphingosine (Cer(d18:1/18:0)) is an amide compound widely found in eukaryotic organisms that enhances protein phosphatase 2A (PP2A) activity by interfering with the binding of PP2A to PP2A inhibitor 2, leading to dephosphorylation of Akt.N-Stearoylsphingosine is used in prostate cancer research.