PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand, Blue: CRBN Ligand, Black: Linker, E3 ligase ligand-linker conjugate).

PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma. (Pink: BRD4 ligand ; Blue: Ligands for E3 Ligase E3 ligase ligand; Black: linker).

PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research. (Pink: BRD3 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.

PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research. (Pink: Bcr-Abl ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma. (Pink: BCL6 ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC Akt3 Degrader-1 is a highly efficient and selective PROTAC degrader targeting Akt3. PROTAC Akt3 Degrader-1 shows weak antiproliferative activity in 36 cell lines. PROTAC Akt3 Degrader-1 can be used for the study of Triple-negative breast cancer and melanoma. (Pink: Akt3 ligand ; Blue: Cereblon ligand ; Black: linker).

Proquinazid is a Bcl-2 and PCNA modulator, oxidative stress inducer, genotoxin and apoptosis inducer. Proquinazid causes DNA damage and also triggers apoptosis by regulating pro-apoptotic and anti-apoptotic proteins.

PRMT5-MTA-IN-7 (Compound 14) is a selective PRMT5-MTA inhibitor. PRMT5-MTA-IN-7 exhibits KD values of PRMT5-MTA-IN-7 for PRMT5-MTA and PRMT5-SAM of 236 nM and 2.84 μM respectively, and the IC50 values of 4.08 and 13.6 μM respectively. PRMT5-MTA-IN-7 can selectively inhibit the proliferation of MTAP-deficient cancer cells. PRMT5-MTA-IN-7 can be used for the study of colon cancer.

PPI stabilizer-1-1 (Compound 2) is a KRAS dimerizing agent. PPI stabilizer-1-1 dimerizes KRAS with a KD of 3.8 µM. PPI stabilizer-1-1 co-crystallizes with GCP-KRASG12D. PPI stabilizer-1 can be used for the research of kras-driven cancers.

PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC50 = 1.51 μM), PPARδ (EC50 = 1.11 μM), and PPARγ (EC50 = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/ Streptozotocin (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes.

PNA5 is a novel, blood-brain barrier permeable glycosylated angiotensin-(1-7) peptide and MasR agonist. PNA5 inhibits IL-7, increases IL-10. PNA5 inhibits ROS generation, decreases Iba-1 expression. PNA5 exhibits sustained cognitive protective effects. PNA5 rescues blunted cerebral functional hyperemia. PNA5 can be used in the research of inflammation-related brain diseases.

pKal-IN-1 (compound 13) is a plasma kallikrein (pKal) inhibitor. pKal-IN-1 can be used for the research of diabetic macular edema, diabetic retinopathy.

PJ17 is a potent dual-target inhibitor of AChE and GSK-3β, with IC50 values of 8.84 μM and 4.19 μM, respectively. PJ17 shows no significant neurotoxic effect in primary cerebellar granule neuron cultures. PJ17 serves as a template for the design of multitarget drugs. PJ17 can be used for the research of Alzheimer's disease.

Piquindone (Ro 22-1319) is a potent antipsychotic agent. Piquindone binds to a D2 dopaminergic receptor subtype in a sodium-dependent manner. Piquindone can be used in the research of schizophrenia.

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.

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.

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.

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.

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.

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.

PDE4-IN-33 is a phosphodiesterase 4 (PDE4) inhibitor. PDE4-IN-33 reduces uric acid levels. PDE4-IN-33 PDE4-IN-33 can be used for the research of hyperuricemia and gout.

PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.

PDE1-IN-12 (P78, the first compound in 12) is a PDE1 inhibitor. PDE1-IN-12 inhibits PDEl-mediated suppression of the dopamine D1 receptor intracellular pathway and can be used for narcolepsy.

PDE1-IN-11 (Compound 5cc) is an orally active and highly selective PDE1A1 inhibitor. PDE1-IN-11 increases intracellular cAMP and cGMP levels, activating the PKA-CREB and NO-cGMP-PKG signaling pathways, promoting osteoblast differentiation and bone formation, while suppressing osteoclastogenesis and bone resorption. PDE1-IN-11 is promising for research of postmenopausal osteoporosis (PMO) and other bone metabolism disorders.

PAT-347 sodium is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood.

PAT-078 is a type II autotaxin (ATX) inhibitor. PAT-078 mainly occupies the hydrophobic pocket of ATX, blocks the bottleneck region between the hydrophobic channel and the catalytic site, and does not interact with the zinc ion at the catalytic site.

PARP1-IN-56 (Compound RCY) is an I-labeled poly(ADP−ribose) polymerase (PARP1) inhibitor. PARP1-IN-56 can be radiolabeled with 211At or 125I for use as an α-emitting radiotherapeutic agent. PARP1-IN-56 can be used for the research of cancer.

PARP1-IN-53 (Compound 328) is a quinazolinone derivative and PARP1 inhibitor with a PARP1 IC50 of 0.1 nM and selectivity over PARP2, which has a PARP2 IC50 of 23 nM.PARP1-IN-53 can be used for the research of cancer.