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.

Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.

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.

SU3327 (halicin) is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 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

MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 inhibitor with antitumor activity.

TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.

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.

β-catenin/BCL9 PPI-IN-1 (compound B4) is an effective inhibitor of the interaction between β-catenin and B-cell lymphoma 9 proteins (β-catenin/BCL9 PPI), with an IC50 value of 2.25 μM.

eIF4E/eIF4G PPI-IN-1 is an inhibitor that disrupts the interaction between eIF4E and eIF4G, exhibiting a dissociation constant (KD) of 20.2 μM for the eIF4E protein. It demonstrates antitumor effects through various mechanisms, including modulation of eIF4E activity via inhibition of the Ras/MAPK/eIF4E signaling pathway, influencing apoptosis and cell migration. Additionally, eIF4E/eIF4G PPI-IN-1 inhibits the growth of HepG2 xenografted tumors in nude mice and is relatively non-toxic to mice.

SHOC2–RAS PPI-IN-1 (compound 6) is a non-covalent competitive inhibitor that targets the interaction between SHOC2 and RAS proteins. It exhibits an IC50 of 0.048 μM and a KD of 0.065 μM against NRASQ61R. This compound inhibits SMP phosphatase-complex activity, increasing CRAFS259 phosphorylation levels and thus blocking the MAPK signaling pathway (by reducing pMEK and pERK levels). It induces cell cycle arrest and apoptosis in tumor cells. SHOC2–RAS PPI-IN-1 is used in targeting studies for malignancies, such as NRASQ61R-mutant melanoma and colorectal cancer.

XIAP-CASP7 PPI-IN-1 is a reversible inhibitor of the XIAP:CASP7 interaction, effectively disrupting the connection between XIAP and CASP7. It selectively induces apoptosis in MCF-7 and caspase-3 low-expression (CASP3/DR) triple-negative breast cancer cells. The compound overcomes chemoresistance by down-regulating β-catenin and associated ABC transporters in paclitaxel-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 is useful for breast cancer research.

PEX5-PEX14 PPI-IN-3 (Compound 7) is an inhibitor of the PEX5-PEX14 protein-protein interaction, with an EC50 of 95 μM. It demonstrates an EC50 of 7.2 μM against Trypanosoma brucei and exhibits low cytotoxicity in HepG2 cells. PEX5-PEX14 PPI-IN-3 also possesses antiparasitic activity.

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].