| 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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Frontiers in Immunology, May 25, 2022, 861292
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Circulation Research, March 27, 2026, e327680
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Anticancer Research, March 2023, 1103-1112
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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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| S8987 |
Batoprotafib (TNO155)
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Batoprotafib (TNO155) is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM, and has potential antineoplastic activity.
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bioRxiv, March 11 2026, nan
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Molecular Cancer Therapeutics, December 01 2023, 1479-1492
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Journal of Thoracic Oncology, August 2021, 1321-1332
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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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Journal of Biomedical Science, 2025, 88
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Cell Death & Disease, 2025, 864
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| S1949 |
Menadione (Vitamin K3)
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Menadione (Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
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mSphere, 2025, 10(1):e0070324
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Med -N Y, 2022, S2666-6340-2200365-8
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Mol Cell, 2021, S1097-2765(21)00269-0
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