ppi

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Pantoprazole (BY1023) is a proton pump inhibitor used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

IPR-803 is an effective inhibitor of the uPAR·uPA protein-protein interaction (PPI) with anti-tumor activity. IPR-803 binds directly to uPAR with a Ki of 0.2 μM.

Rabeprazole sodium (Habeprazole Sodium) is a 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of stomach ulcers and Zollinger-Ellison syndrome. The drug inhibits H(+)-K(+)-exchanging ATPase which is found in gastric parietal cells.

BMS-8 is a novel inhibitor of the PD-1/PD-L1 interaction (IC50: 7.2 μM) by binding directly to PD-L1 and inducing the formation of PD-L1 homodimers.

M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential proteinprotein interaction (PPI) within the SAC. It can disturbs conformational dynamics of Mad2 critical for complex formation with Cd

HIV-1 Nef-IN-1 is an inhibitor of the HIV-1 Nef protein, effectively competing for Nef-SH3Hck interactions (Kd: 6.7 μM).

SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction, with an IC50 of 2 μM.

PPI-1019 is an APP (β-amyloid A4) inhibitor for the treatment of neurological disorders and the study of Alzheimer's disease (AD).

PPI-1040 is an innovative ethyl ether phospholipid compound. When used concurrently with the same dosage of the ether lipid precursor PPI-1011, it does not effectively elevate phospholipid levels or reduce hyperactivity. Conversely, treatment with PPI-1040 effectively normalizes hyperactive behavior in mice.

ATXN1-MED15 PPI-IN-1 is an inhibitor of the ATXN1/MED15 interaction. It binds to residues 99 to 163 of ATXN1, disrupting the interaction between ATXN1 and MED15, as well as the dimerization of polyQ-expanded ATXN1. This compound is applicable for research related to Spinocerebellar Ataxia Type 1.

PPI-2458 is a synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class.

PRMT5:MEP50 PPI, a pioneering inhibitor of the PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI), demonstrates anti-tumor and anti-proliferative effects in lung and prostate cancer cells.

PEX5-PEX14 PPI-IN-1 (Compound 8) is a PEX14-PEX5 protein-protein interaction (PPI) inhibitor with an inhibitory constant (Ki) of 53 μM that disrupts the interaction between PEX5 and TbPEX14. It effectively inhibits the bloodstream form of Trypanosoma brucei brucei with a half-maximal effective concentration (EC50) of 5 μM [1].

Compound 12, also known as PEX5-PEX14 PPI-IN-2, is a PEX14-PEX5 protein-protein interaction (PPI) inhibitor with half-maximal effective concentration (EC50) values of 5 µM in T. b. brucei and 17 µM in HepG2 cells. It is utilized in the study of diseases associated with trypanosome infection [1].

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

KEAP1-NRF2PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. In DNA damage tests, its IC50 values are 136 nM in human TK6 cell lines and 62 nM in insect SF9 cell lines.

PPIase-Parvulin Inhibitor is a cell-pemeable inhibitor of the Pin1 and Pin4.

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with antidepressant and anxiolytic-like effects.

PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0 G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.

DPPI 1c hydrochloride is an inhibitor of dipeptidyl peptidase IV (IC50 = 104 nM) that shows selectivity over enzymes with DPP-like activity (IC50 > 30 μM).

Poloppin is a protein-protein interactions modulator of the mitotic polo-like kinases that acts by targeting mutant KRAS. It works synergistically with Crizotinib, an inhibitor of the c-MET receptor, against mutant KRAS-expressing cancer cells.

3-MPPI was a high-affinity nonselective α1-antagonist.

Bractoppin is a drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem (t)BRCT domain (IC50 = 0.074 μM), which selectively inhibits substrate binding with nanomolar potency in vitro. Structure-activity exploration suggests that Bractoppin engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket that is distinct in structurally related BRCT domains, conferring selectivity.