PIN1 degrader-2 (compound 164A10) is a potent and selective covalent PIN1 degrader (IC50 = 4.1 nM) that induces PIN1 degradation in cancer cells (DC50 < 500 nM). PIN1 degrader-2 can be used for cancer research.

PIM-IN-3 (Compound 50) is an orally active new anti-intestinal worm drug. PIM-IN-3 exhibits strong inhibitory activity in vitro, especially for whipworms (IC50 = 6.6 µM). PIM-IN-3 has low cytotoxicity. PIM-IN-3 can be used in the research of gastrointestinal nematode diseases.

Picenadol (LY-150720) hydrochloride is an opioid mixed agonist-antagonist analgesic. Picenadol hydrochloride is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol hydrochloride has anticholinergic activity.

PI3Kδ-IN-27 is an PI3Kδ inhibitor with an IC50 of 355.3 nM. PI3Kδ-IN-27 exhibits anti-SARS-CoV-2 activity. PI3Kδ-IN-27 can be used for the research of infection, such as COVID-19.

PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer.

PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.

PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer.

PI3K/PIKK-IN-2 (compound 2) is an inhibitor of PI3K/PIKK. PI3K/PIKK-IN-2 can be used in preparing antibody-drug conjugates (ADCs).

PI3K/PIKK-IN-1 is a PI3K and PIKK inhibitor that serves as a payload for antibody-drug conjugates (ADC) to prepare ADC. PI3K/PIKK-IN-1 is applicable to research related to breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer.

PI3K/AKT-IN-5 (Compound 3h) is a PI3K/AKT inhibitor. PI3K/AKT-IN-5 exhibits outstanding broad-spectrum anti-cancer activity, especially being sensitive to colorectal cancer. PI3K/AKT-IN-5 significantly reduces cell colony formation, induces G2/M phase cell cycle arrest and cell apoptosis. PI3K/AKT-IN-5 can be used for research on colorectal cancer.

PI3K/AKT/ERK/CREB activator 1 is an orally active PI3K/AKT/ERK/CREB pathway activator. PI3K/AKT/ERK/CREB activator 1 maintains neuronal survival and function, promotes neuronal proliferation, restores the viability of damaged neurons, and facilitates synapse formation. PI3K/AKT/ERK/CREB activator 1 alleviates neuroinflammation by reducing the levels of pro-inflammatory cytokines, preserves synaptic ultrastructure and restores spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB activator 1 can be used in research related to Alzheimer's disease.

Phosphonoformyl-CMP (CMP-5'-Phosphonoformic acid) is a nucleoside metabolite.

Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia. (Pink: Bcr-Abl ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).

Phenylaminojuglone AJ-2 is a nitric oxide synthase inhibitor that interacts with soluble guanylate cyclase, β-adrenergic receptor, CaV1.2 calcium channel, KV channel and KCa channel. Phenylaminojuglone AJ-2 blocks extracellular Ca2+ influx, regulates the activity of the NO−sGC−cGMP signaling pathway, and inhibits pharmacologic and electromechanical contractions of smooth muscle. Phenylaminojuglone AJ-2 is applicable to studies related to intestinal spasm.

Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases.

Phenamacide hydrochloride is an anti-spasmodic agent that can be used for the study of urinary incontinence.

PHD-1-IN-4 is a brain-penetrant PHD-1 inhibitor with an IC50 of 0.074 μM.

PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC50 of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury.

PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.

PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research.

PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.

PF-07245303 is a ITK/TRK inhibitor. PF-07245303 reduces the production of inflammatory cytokines such as IL-4 and IFNγ, and inhibits the phosphorylation of PLCγ1. PF-07245303 inhibits nerve growth factor-induced basophil activation and the phosphorylation of TRKA. PF-07245303 reduces oxazolone-induced ear swelling in mouse ear tissues. PF-07245303 is applicable to research related to atopic dermatitis.

PF-03246799 monohydrochloride is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 monohydrochloride shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 monohydrochloride has the potential for stress urinary incontinence (SUI) research.

Perrimustine is a cysteamine (CysA) derivative with potent antitumor activity. Perrimustine exhibits significant effect on B16 melanoma and metastasized melanoma cells by causing DNA damage. Perrimustine exhibits antitumor effects in mice bearing various cancers, including lung carcinoma, leukemia, lymphoma, melanoma, colon carcinoma, and glioma. Perrimustine can be used for cancer research, such as melanoma and leukemia.

Periplocoside O is a natural steroid.

Penisimplicissin is a funicone-like compound and antiviral agent. Penisimplicissin reduces the expression of AhR and viral nucleocapsid protein. Penisimplicissin improves the cell viability and morphological characteristics of CCoV-infected cells. Penisimplicissin inhibits CCoV infection. Penisimplicissin can be used in studies related to canine coronavirus infection.

Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus.

PD-L1-IN-8 is a PD-L1 inhibitor (IC50 = 0.89 nM). PD-L1-IN-8 shows low CYP inhibition and minimal hERG activity. PD-L1-IN-8 can be used for the study of colon cancer.

PDL1 degrader-3 (comppund e24) is a CSN5-binding antitumor immunomodulator with a human CSN5 Kd of 4.53 μM. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer.

PDI-IN-5 (compound 30z) is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI) with a 2-chloro-pyrrolopyrimidin-4-one scaffold, with an IC50 of 0.4 μM. PDI-IN-5 exhibits selectivity for ERp57 and GPX4, and inhibits glioblastoma. PDI-IN-5 can be used in glioblastoma-related research.