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].

References:

[1]. Yeh ES, et al., PIN1, the cell cycle and cancer. Nat Rev Cancer. 2007 May;7(5):381-8. [Content Brief]

[2]. Lu KP, et al., The prolyl isomerase PIN1: a pivotal new twist in phosphorylation signalling and disease. Nat Rev Mol Cell Biol. 2007 Nov;8(11):904-16. [Content Brief]

PIN1 Related Products (20)
Antibodies (2)

By Effects:	Inhibitors (15) Degraders (3) Modulator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-139361

Sulfopin	Inhibitor	99.69%
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent K_i 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.

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 K_i value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer.

HY-128034

PPIase-Parvulin inhibitor	Inhibitor	99.79%
PPIase-Parvulin inhibitor (compound B) is a cell-permeable inhibitor targeting PPIase Pin1 and Par14, with IC_{50_s} 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).

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.

HY-P4359

Suc-AEPF-AMC	Inhibitor	98.67%
Suc-AEPF-AMC is a peptide substrate of Pin1 and Par14 peptidyl prolyl isomerase.

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.

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.

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.

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.

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.

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.

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.

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 K_D 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.

HY-168872

API32	Inhibitor
API32 is a potent Pin1 inhibitor. API32 interactes with the Pin1 PPIase domain. API32 inhibits cell proliferation and migration. API32 has the potential for the research of hepatocellular carcinoma (HCC).

HY-170429

BJP-07-017-3	Inhibitor
BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC₅₀ of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation.

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.

HY-129310

PIN1 inhibitor 5	Inhibitor
PIN1 inhibitor 5 (compound 7) is a PIN1 inhibitor (K_i=0.08 μM) ,which can be used in cancer research.

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).

HY-W843265

PIN1 inhibitor 6	Inhibitor
PIN1 inhibitor 6 (compound 38) is a Pin1 inhibitor. PIN1 inhibitor 6 can be utilized in cancer research.

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PIN1

PIN1 Related Products (20)

Antibodies (2)

PIN1 Related Products (20):