2. Signaling Pathways
  3. PI3K/Akt/mTOR
  4. PIN1

PIN1

peptidylprolyl cis/trans isomerase, NIMA-interacting 1

PIN1 is a peptidyl-prolyl isomerase (PPIase) that specifically recognizes the pSer/Thr-Pro motif, catalyzes the cis and trans isomerization of the proline amide bond, changes the conformation of the substrate protein, thereby affecting its function, stability or intracellular localization. PIN1 regulates cell cycle proteins such as cyclin D, cyclin E, and CDC25, thereby regulating the G1-S process and mitotic progression. PIN1 regulates the stability of proteins such as p53 and p73, responds to stress signals such as DNA damage, and thus affects cell cycle arrest or apoptosis. PIN1 regulates the phosphorylation of tau protein, mediating the neurological functions. PIN1 regulates transcription factors such as NF-κB and JUN, mediates immune responses. PIN1 dysfunction could lead to Alzheimer's disease, cancer, asthma, or microbial infection[1][2].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-139361
    Sulfopin
    		Inhibitor 99.82%
    Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.
    Sulfopin
  • HY-123847
    KPT-6566
    		Inhibitor 98.0%
    KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer.
    KPT-6566
  • HY-N6924
    Zingibroside R1
    		Inhibitor 99.75%
    Zingibroside R1 is an orally active triterpene saponin with multiple biological activities including antioxidant, anti-inflammatory, antiviral, and metabolic regulatory properties. Zingibroside R1 reduces the expression of PIN family members, inhibits the expression of PLT1/PLT2, WOX5, SHR, and SCR, disrupts auxin transport and distribution, triggers plant ROS responses, and inhibits root growth. Zingibroside R1 extends the lifespan of Caenorhabditis elegans, enhances its heat stress resistance, and improves its motor ability. Hydrogel derivatives of Zingibroside R1 inhibit the proliferation of Candida albicans by binding to its β-1,3-glucan and exhibit antifungal activity. Zingibroside R1 inhibits GLUT1-mediated uptake and alleviates liver injury. Zingibroside R1 can be used in research related to neurodegenerative diseases, vulvovaginal candidiasis, acute liver injury, Ehrlich ascites tumor and HIV-1 infection.
    Zingibroside R1
  • HY-128034
    PPIase-Parvulin inhibitor
    		Inhibitor
    PPIase-Parvulin inhibitor (compound B) is a cell-permeable inhibitor targeting PPIase Pin1 and Par14, with IC50s of 1.5 and 1.0 µM, respectively. PPIase-Parvulin inhibitor has anticancer activity and inhibits the growth and proliferation of mouse embryonic fibroblasts (MEFs).
    PPIase-Parvulin inhibitor
  • HY-168037
    PROTAC PIN1 degrader-1
    PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer.
    PROTAC PIN1 degrader-1
  • HY-168037A
    PROTAC PIN1 degrader-1 TFA
    		Degrader
    PROTAC PIN1 degrader-1 TFA is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer.
    PROTAC PIN1 degrader-1 TFA
  • HY-179577
    PIN1 degrader-3
    		Degrader
    PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50 = 4.65 nM) degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability, with EC50 values after 72 h of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines.PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer.
    PIN1 degrader-3
  • HY-164896
    PIN1 degrader-2
    		Degrader
    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.
    PIN1 degrader-2
  • HY-168038
    PIN1 ligand-1
    		98.40%
    PIN1 ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PIN1 ligand-1 can be used for synthesis PROTAC PIN1 degrader-1 (HY-168037).
    PIN1 ligand-1
  • HY-171334
    (Rac)-P1D-34
    		Degrader 99.45%
    PROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC50 values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively.
    (Rac)-P1D-34
  • HY-P4359
    Suc-AEPF-AMC
    		Inhibitor 98.67%
    Suc-AEPF-AMC is a peptide substrate of Pin1 and Par14 peptidyl prolyl isomerase.
    Suc-AEPF-AMC
  • HY-153675
    BCPA
    		Modulator 98.51%
    BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research.
    BCPA
  • HY-128592
    TAB29
    		Inhibitor
    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.
    TAB29
  • HY-171334A
    P1D-34
    		Degrader
    P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).
    P1D-34
  • HY-143903
    ZL-Pin13
    		Inhibitor
    ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells.
    ZL-Pin13
  • HY-170766
    PIN1 inhibitor 4
    		Inhibitor
    PIN1 inhibitor 4 (compound 6a) is a covalent inhibitor of peptidyl-prolyl isomerase Pin1, with IC50=3.15 μM.
    PIN1 inhibitor 4
  • HY-171442
    PIN1 ligand-2
    		Degrader
    PIN1 ligand-2 (Intermediate M6) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PIN1 ligand-2 can be used for synthesizing PROTACT (Rac)-P1D-34 (HY-171334).
    PIN1 ligand-2
  • HY-164895
    PIN1 degrader-1
    		Degrader
    PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research.
    PIN1 degrader-1
  • HY-137122
    3-Pyridine toxoflavin
    		Inhibitor
    3-Pyridine toxoflavin (compound 49) is a PIN1 inhibitor. 3-Pyridine toxoflavin can be used for the research of immune disease proliferative disorder.
    3-Pyridine toxoflavin
  • HY-143902
    ZL-Pin01
    		Inhibitor
    ZL-Pin01 is a high potent covalent Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) inhibitor. ZL-Pin01 shows potent disruption of the Pin1-substrate interaction with an IC50 of 1.33 μM.
    ZL-Pin01
Cat. No. Product Name / Synonyms Application Reactivity