| E1207 |
Osunprotafib (ABBV-CLS-484)
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Osunprotafib (ABBV-CLS-484) is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity.
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| S5003 |
FK506 (Tacrolimus)
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Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
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Proc Natl Acad Sci U S A, 2025, 122(4):e2418317122
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J Nanobiotechnology, 2025, 23(1):32
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PLoS Pathog, 2025, 21(1):e1012872
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| S2286 |
Cyclosporin A
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Cyclosporin A, a non-polar cyclic oligopeptide, is an immunosuppressive agent that binds to cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay. Cyclosporin A is generally given following transplant surgery to prevent rejection and has been used to test its toxic effect on a perfused 3D proximal tubule model.Cyclosporin A (NSC 290193) can be used to induce animal models of Chronic Rejection of Liver Transplantation.
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Signal Transduct Target Ther, 2025, 10(1):81
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Signal Transduct Target Ther, 2025, 10(1):167
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Adv Sci (Weinh), 2025, 12(36):e06150
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| S8278 |
SHP099 Hydrochloride
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SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50 value of 0.071 μM and shows no activity against SHP1.
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Cancers (Basel), 2025, 17(7)1152
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EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
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Pharmacol Res, 2024, 201:107096
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| S8718 |
RMC-4550
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RMC-4550 is a potent SHP-2inhibitor with an IC50 of 1.55 nM and this compound has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels.
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Nat Cancer, 2025, 10.1038/s43018-025-00960-z
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Cancer Res, 2025, 10.1158/0008-5472.CAN-24-3819
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iScience, 2025, 28(9):113374
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| S6388 |
SHP099
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SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50 value of 71 nM and shows no activity against SHP1.
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iScience, 2025, 28(2):111662
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Res Sq, 2025, rs.3.rs-7032881
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bioRxiv, 2025, 2025.06.11.659120
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| S1514 |
Cyclosporine
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Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
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J Adv Res, 2024, S2090-1232(24)00499-5
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Cells, 2023, 12(23)2696
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Int J Mol Sci, 2023, 24(11)9708
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| S3620 |
β-Glycerophosphate sodium salt hydrate
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β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor.
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Nat Commun, 2024, 15(1):2384
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Discover Oncology, 2024, 338
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Discov Oncol, 2024, 15(1):338
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| S4007 |
Pentamidine isethionate
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Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.
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Nat Commun, 2022, 13(1):6323
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Biomed Chromatogr, 2022, e5519.
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Cell Prolif, 2020, 53(1):e12718
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| S7573 |
GSK2830371
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GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
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J Biomed Sci, 2025, 32(1):88
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Cancer Res, 2022, canres.4145.2021
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Cancer Res, 2022, 82 (12): 2313–2326.
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