2. PI3K/Akt/mTOR
  3. PIN1

PIN1

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].

PIN1 Related Products (23):

Cat. No. Product Name Effect Purity
  • 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[1].
  • HY-123847
    KPT-6566 Inhibitor
    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[1].
  • HY-139361
    Sulfopin Inhibitor 99.69%
    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[1].
  • HY-128034
    PPIase-Parvulin inhibitor Inhibitor 99.79%
    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)[1].
  • HY-171334
    (Rac)-P1D-34 Degrader
    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[1].
  • 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)[1].
  • HY-RS23468
    Pin1 Rat Pre-designed siRNA Set A
    Pin1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pin1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
  • HY-171442A
    (R)-PIN1 ligand-2
    (R)-PIN1 ligand-2 is a PIN1 ligand, and can be used for synthesis of PROTACs, such as P1D-34 (HY-171334A)[1].
  • 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[1].
  • HY-12135
    Poloxipan Inhibitor
    Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC50 values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research[1].
  • 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[1].
  • HY-129310
    PIN1 inhibitor 5 Inhibitor
    PIN1 inhibitor 5 (compound 7) is a PIN1 inhibitor (Ki=0.08 μM) ,which can be used in cancer research[1].
  • 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)[1].
  • 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[1].
  • HY-P4359
    Suc-AEPF-AMC Inhibitor 98.67%
    Suc-AEPF-AMC is a peptide substrate of Pin1 and Par14 peptidyl prolyl isomerase[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[1].
  • 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[1].
  • HY-168037
    PROTAC PIN1 degrader-1
    PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part)[1].
  • HY-168036
    PIN1 inhibitor 3 Inhibitor
    PIN1 inhibitor 3 (Compound A0) is a PIN1 inhibitor, with a KD of 25 nM and an IC50 of 150 nM. PIN1 inhibitor 3 can be used as a target protein ligand for the synthesis of PROTAC. PIN1 inhibitor 3 can be utilized in cancer research[1].
  • 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[1].