pin1

PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM) that retains the active conformation of pXPO5, restoring its ability to transport pre-miRNAs from the nucleus to the cytoplasm, thereby up-regulating anticancer miRNA biogenesis to suppress hepatocellular carcinoma development both in vitro and in vivo. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain, effectively inhibiting Pin1 cis-trans isomerizing activity.

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

Sulfopin is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17nM. Sulfopin blocks Myc-driven tumors in vivo.

Suc-AEPF-AMC (Suc-Ala-Glu-Pro-Phe-AMC) is a peptide substrate for the peptidyl prolyl isomerases Pin1 and Par14, and is a peptide compound that can be used to assay protease activity.

BCPA is a non-cytotoxic Pin1 modulator.BCPA modulates osteoclast activation and attenuates the reduction of Pin1 protein, thereby inhibiting RANKL-induced receptor activators of osteoclastogenesis.BCPA is used in the study of osteoporosis.

PROTAC PIN1 degrader-1, a targeted PROTAC for PIN1, effectively degrades PIN1 protein in MDA-MB-468 triple-negative breast cancer cells with a DC50 value of 0.018 μM. This compound is utilized in tumor research.

PIN1 inhibitor3 (Compound A0) is a PIN1 inhibitor with a dissociation constant (KD) of 25 nM and a half-maximal inhibitory concentration (IC50) of 150 nM. It serves as a target protein ligand for PROTAC synthesis and is applicable in cancer research.

PIN1degrader-1 (Compound 158H9) is an inhibitor of the peptidyl-prolyl cis-trans isomerase (Pin1), with an IC50 of 21.5 nM. It covalently binds to Cys113 on Pin1, inducing conformational changes that decrease the protein's stability and lead to proteasome-dependent degradation. PIN1degrader-1 also inhibits the viability of various cancer cells, making it useful for cancer research.

PIN1 inhibitor6 (compound 38) is a Pin1 inhibitor utilized in cancer research.

PIN1 inhibitor4 (compound 6a) is a covalent inhibitor of the enzyme peptidyl-prolyl cis-trans isomerase Pin1, with an IC50 value of 3.15 μM.

(R)-PIN1 ligand-2 is a PIN1 ligand that can be utilized in the synthesis of PROTACs, such as P1D-34.

PIN1 inhibitor 2 (compound 12) is a potent inhibitor of PIN1, demonstrating significant antitumor activity with an IC50 of 9.55 μM against MCF7 cells, making it a promising candidate for breast cancer research [1].

Pin1 modulator 1 (compound IIb-219) is a specific β-Catenin targeting agent that inhibits the Wnt pathway and is applicable in researching Wnt-mediated diseases, including cancer [1].

PIN1ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It can be utilized in synthesis processes.

PIN1ligand-2 (Intermediate M6) is a ligand designed for PROTAC target proteins (Ligands for Target Protein for s). It can be utilized in the synthesis of PROTACT(Rac)-P1D-34.

ZL-Pin13 is a potent covalent inhibitor of cellular activity that selectively acts on Pin1 (IC50: 67 nM). ZL-Pin13 effectively inhibits the proliferation of MDA-MB-231 cells and downregulates Pin1 substrates.

PPIase-Parvulin Inhibitor is a cell-pemeable inhibitor of the Pin1 and Pin4.

Juglone (Regianin) is a natural naphthoquinone found in the black walnut (J. nigra) and other plants in the Juglandaceae family. Juglone also irreversibly inhibits peptidyl-prolyl cis trans isomerases of the parvulin family, including human Pin1, yeast Ess1 Ptf1, and E. coli parvulin (Ki = 55.9 nM). Juglone also blocks transcription by RNA polymerases I, II, and III (IC50s = 2-7 μM) and attenuates kidney fibrosis in rats treated with unilateral ureteral obstruction, both through Pin1-independent mechanisms.

TAB29 is a potent peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) inhibitor (IC50 of 874 nM), with therapeutic potential for human cancers.

amyloid P-IN-1 can be used in studies about diseases with depletion of serum amyloid P components such as Alzheimer's disease, amyloidosis, osteoarthritis, and type 2 diabetes mellitus.

Thalidomide-O-C5-piperidine-NH-Boc serves as an E3 Ligase Ligand-Linker Conjugate. This compound is utilized in the synthesis of PROTAC PIN1 degrader-1.

BJP-07-017-3 is an inhibitor of proline cis-trans isomerase (Pin1) with an IC50 of 9 nM. It forms a covalent bond with Cys113 of Pin1, inducing conformational changes that decrease its stability and lead to proteasome-dependent degradation.

API32 is a potent Pin1 inhibitor that interacts with the Pin1 PPIase domain. It effectively suppresses cell proliferation and migration, making it a promising candidate for research in hepatocellular carcinoma (HCC).

PROTACPIN1degrader-2 (1) is a PROTAC degrader of PIN1. The IC50 values of PROTACPIN1degrader-2 (1) against various cancer cells are as follows: 2248 nM for MV-4-11 cells, 3984 nM for MOLM-13 cells, and 3925 nM for HL-60 cells.