PIN1 Inhibitor

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.

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.

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.

PPIase-Parvulin inhibitor (compound B) is a cell-permeable inhibitor targeting PPIase Pin1 and Par14, with IC_50s 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).

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

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.

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.

PIN1 inhibitor 4 (compound 6a) is a covalent inhibitor of peptidyl-prolyl isomerase Pin1, with IC₅₀=3.15 μM.

3-Pyridine toxoflavin (compound 49) is a PIN1 inhibitor. 3-Pyridine toxoflavin can be used for the research of immune disease proliferative disorder.

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.

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.

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).

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.

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.

L-Balenine is an orally active Pin1 inhibitor and intracellular pH buffer. L-Balenine enhances the phagocytic activity of macrophages, and promotes the expression of pro-inflammatory and anti-inflammatory cytokines during muscle degeneration. L-Balenine also upregulates the expression of myogenic marker genes associated with regeneration, thereby effectively driving skeletal muscle regeneration. L-Balenine can be widely used in studies related to skeletal muscle injury and its repair mechanisms.

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

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