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PIN1 inhibitors block a prolyl isomerase that recognizes phosphorylated serine-proline motifs. Protein interacting with never in mitosis A 1 (PIN1) was identified in 1996 as a human isomerase required for the regulation of mitosis. A 1997 study showed that it isomerizes the peptide bond before proline only when the preceding serine or threonine is phosphorylated. By switching the conformation of phosphoproteins, PIN1 links proline-directed kinase signaling to protein stability, localization and activity. It is studied in cancer biology, cell cycle control and neurodegeneration. Sulfopin and KPT-6566 bind the enzyme covalently, and ZL-Pin13 and TAB29 are further PIN1 inhibitors. Suc-Ala-Glu-Pro-Phe-pNA is a chromogenic peptide substrate used in isomerase assays.
TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874 nM, possesses therapeutic potential for human cancers.
KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
Synonyms: Suc-AEPF-pNA
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc.
Synonyms: PIN1-3
Sulfopin is a selective covalent inhibitor of Pin1, exhibiting an apparent Ki of 17 nM. This inhibitor effectively disrupts Myc-driven tumor growth in vivo. By targeting the peptidyl-prolyl isomerase Pin1, sulfopin plays a significant role in modulating oncogenic activity and tumor suppressor function, making it a valuable tool for cancer research.
BCPA is a selective modulator of the peptidyl-prolyl isomerase Pin1. It effectively inhibits receptor activator of nuclear factor kappa-B ligand (RANKL)-induced osteoclastogenesis by preventing the reduction of Pin1 protein levels. BCPA is a valuable tool for research in osteoporosis, as it modulates osteoclast activation without exhibiting cytotoxic effects.
ZL-Pin13 is a highly potent covalent inhibitor of Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1), exhibiting an IC50 value of 67 nM. This compound effectively inhibits cell proliferation and downregulates Pin1 substrates in MDA-MB-231 breast cancer cells. ZL-Pin13 is a valuable tool for studying the role of Pin1 in cellular processes and may contribute to the development of therapeutic strategies targeting cancer progression.
3-Pyridine toxoflavin is a potent inhibitor of the prolyl isomerase PIN1. This compound demonstrates key biological activity by modulating protein-protein interactions and cellular signaling pathways implicated in immune disease and proliferative disorders. Research applications include the investigation of mechanisms underlying cellular proliferation and potential therapeutic strategies for immune-related conditions.
ZL-Pin01 is a potent covalent inhibitor of Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) that effectively disrupts Pin1-substrate interactions. With an IC50 value of 1.33 μM, ZL-Pin01 serves as a valuable tool for investigating the role of Pin1 in various biological processes. This compound is particularly useful in research focused on cellular signaling, protein folding, and disease mechanisms associated with Pin1 dysregulation.
PIN1 Inhibitor 3 is a selective inhibitor of prolyl isomerase PIN1, exhibiting a dissociation constant (KD) of 25 nM and an IC50 of 150 nM. This compound serves as a valuable tool for investigating the role of PIN1 in various cellular processes and is particularly relevant in cancer research. Additionally, PIN1 Inhibitor 3 can be employed as a ligand in the synthesis of Proteolysis Targeting Chimeras (PROTACs), enabling targeted protein degradation studies.
API32 is a selective inhibitor of the prolyl isomerase Pin1, targeting its PPIase domain. It demonstrates significant activity in inhibiting cell proliferation and migration, making it a valuable tool for studying cellular processes. API32 holds potential for research applications in hepatocellular carcinoma (HCC) and related studies on tumor biology and metastasis.
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BJP-07-017-3 is a potent inhibitor of proline cis-trans isomerase (Pin1) with an IC50 of 9 nM. It covalently modifies the cysteine residue at position 113 of Pin1, causing significant conformational changes that impair its stability. This interaction leads to proteasome-mediated degradation of Pin1, making BJP-07-017-3 a valuable tool for investigating cellular processes regulated by Pin1. It is suitable for research applications focused on cancer and neurodegenerative diseases where Pin1 plays a critical role.
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PIN1 inhibitor 5 is a potent inhibitor of the prolyl isomerase PIN1, with a Ki value of 0.08 μM. This compound is primarily utilized in cancer research to explore the role of PIN1 in tumorigenesis and associated signaling pathways. Its inhibitory effects can aid in the study of cellular processes linked to cancer progression and potential therapeutic strategies.
PIN1 inhibitor 6 is a specific inhibitor of the prolyl isomerase PIN1, which plays a crucial role in regulating cell signaling pathways that influence cancer progression. By hindering PIN1 activity, this compound is valuable for exploring its effects on tumor cell proliferation and survival. It serves as a useful tool in cancer research, particularly in studies aimed at understanding PIN1's role in oncogenic processes and potential therapeutic interventions.
