PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer. (Pink: FSP1 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-37 (compound 16) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 144 nM. PROTAC EZH2 Degrader-37 is applicable to lymphoma-related research. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-36 (compound 15) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 16.00 nM.PROTAC EZH2 Degrader-36 applicable to lymphoma-related research. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-27 is a EZH2 PROTAC inhibitor with an IC50 of 4.00 nM against EZH2. PROTAC EZH2 Degrader-27 inhibits methyltransferase activity by interacting with the SET domain of EZH2. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: ).

PROTAC EZH2 Degrader-25 (compound 10) is an EZH2-targeting PROTAC degrader. PROTAC EZH2 Degrader-25 triggers ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-25 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-24 (compound 9) is an EZH2-targeting PROTAC with EZH2 methyltransferase inhibitory activity. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-20 (compound 54) is an EZH2-target PROTAC degrader with antiproliferative activity and IC50 values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).

PROTAC EZH2 Degrader-15 (compound 5) is an EZH2-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits EZH2 methyltransferase activity. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC EZH2 Degrader-10 (compound 1) is a PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-10 can be used for the research of cancer. (Pink: EZH2 ligand ; Blue: Cereblon ligand ; Black: linker).

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.