S2286 |
Cyclosporin A
|
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. |
-
Cell Rep, 2024, S2211-1247(23)01591-7
-
mSphere, 2024, 9(1):e0055423
-
Food Chem Toxicol, 2024, 188:114665
|
|
S5003 |
Tacrolimus (FK506)
|
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. |
-
Nat Immunol, 2024, 25(5):860-872
-
Int J Antimicrob Agents, 2024, 63(5):107116
-
Cell Commun Signal, 2024, 22(1):428
|
|
S8278 |
SHP099 HCl
|
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. |
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
-
Pharmacol Res, 2024, 201:107096
-
Biomed Pharmacother, 2024, 175:116590
|
|
S8718 |
RMC-4550
|
RMC-4550 is a potent SHP-2inhibitor with an IC50 of 1.55 nM and it has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels. |
-
J Neuroinflammation, 2024, 21(1):37
-
Cell Rep, 2023, 42(6):112570
-
Oncogene, 2023, 42(20):1620-1633
|
|
S6388 |
SHP099
|
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. |
-
MedComm (2020), 2024, 5(4):e527
-
NPJ Precis Oncol, 2023, 7(1):136
-
Front Immunol, 2023, 14:1260545
|
|
S1514 |
Cyclosporine
|
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation. |
-
J Adv Res, 2024, S2090-1232(24)00499-5
-
Cells, 2023, 12(23)2696
-
Int J Mol Sci, 2023, 24(11)9708
|
|
S7573 |
GSK2830371
|
GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
|
-
Cancer Res, 2022, canres.4145.2021
-
Cancer Res, 2022, 82 (12): 2313–2326.
-
iScience, 2022, 25(9):104892
|
|
S1949 |
Menadione (Vitamin K3)
|
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. |
-
Med -N Y, 2022, S2666-6340-2200365-8
-
Mol Cell, 2021, S1097-2765(21)00269-0
-
DNA Repair (Amst), 2021, 105:103152
|
|
S4007 |
Pentamidine isethionate
|
Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein. |
-
Nat Commun, 2022, 13(1):6323
-
Biomed Chromatogr, 2022, e5519.
-
Cell Prolif, 2020, 53(1):e12718
|
|
S3620 |
β-Glycerophosphate sodium salt hydrate
|
β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor. |
-
Nat Commun, 2024, 15(1):2384
-
Discov Oncol, 2024, 15(1):338
-
Res Sq, 2023, rs.3.rs-2405644
|
|
S8182 |
NSC87877
|
NSC-87877 is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1/2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability/proliferation. |
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
-
Inflammation, 2022, 10.1007/s10753-022-01762-6
-
Oncotarget, 2020, 21;11(3):265-281
|
|
S7437 |
Sal003
|
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
-
Front Pharmacol, 2023, 14:1095307
-
bioRxiv, 2023, 2023.05.19.540602
-
bioRxiv, 2023, 2023.05.19.540602
|
|
S8987 |
Batoprotafib(TNO155)
|
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. TNO155 has potential antineoplastic activity. |
-
J Neuroinflammation, 2024, 21(1):37
-
Pharmacol Res, 2024, 201:107096
-
Mol Oncol, 2024, 10.1002/1878-0261.13725
|
|
S6570 |
TPI-1
|
TPI-1 (Tyrosine Phosphatase Inhibitor 1) is a potent inhibitor of SHP-1 with IC50 of 40 nM for recombinant SHP-1. TPI-1 exhibits anticancer activity. |
-
Immunity, 2024, 57(2):287-302.e12
-
Cell Rep Med, 2024, 5(1):101374
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
|
|
S5452 |
Sanguinarine chloride
|
Sanguinarine, a plant alkaloid, is a potent and specific protein phosphatase (PP) 2C inhibitor. Sanguinarine chloride can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB. |
-
Cell Rep, 2023, 42(3):112186
-
Front Pharmacol, 2021, 12:638215
|
|
S1857 |
Etidronate
|
Etidronate is a non-aminobisphosphonate, show protein tyrosine phosphatase (PTP) inhibitory activity, used for the treatment of Paget's disease and the prevention of heterotopic ossification. |
-
J Immunother Cancer, 2020, 8(2)e001037
|
|
S0528 |
Raphin1
|
Raphin1 is an orally bioavailable, selective inhibitor of R15B (PPP1R15B, a regulatory subunit of protein phosphatase 1). Raphin1 binds strongly to the R15B-PP1c holophosphatase with Kd of 33 nM. |
-
Cell Rep, 2024, 43(8):114606
-
Cell Stem Cell, 2022, 29(7):1119-1134.e7
|
|
S2435 |
Sodium stibogluconate
|
Sodium stibogluconate (SSG, Stibogluconate trisodium nonahydrate, Lenocta, VQD-001), a pentavalent antimony derivative, is a potent and selective inhibitor of protein tyrosine phosphatase (PTPase). Sodium stibogluconate inhibits 99% of Src homology 2 domain-containing phosphatase 1 (SHP-1) activity at 10 μg/ml and similar degrees of inhibition of SHP-2 and PTP1B requires 100 μg/ml. Sodium stibogluconate is a drug used in treatment of leishmaniasis. |
-
Gastroenterology, 2024, S0016-5085(24)00062-3
-
Biomed Chromatogr, 2022, e5519.
|
|
S5953 |
Menadione bisulfite sodium
|
Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
-
Life Sci, 2020, 242:117159
|
|
S3678 |
PTP Inhibitor II
|
PTP Inhibitor II (NSC 129010, 4-(Bromoacetyl)anisole) is a cell-permeable protein tyrosine phosphatase (PTP) inhibitor that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with Ki value of 128 μM. |
-
Fish Shellfish Immunol, 2020, 99:562-571
|
|
S7485 |
CCT007093
|
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. |
-
Oncogene, 2016, 35(42):5552-5564
|
|
S0136 |
KY-226
|
KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. |
-
J Immunol, 2022, 209(9):1662-1673
|
|
S5595 |
3-Carene
|
3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. |
-
Phytomedicine, 2021, 91:153707
|
|
S6777 |
NSC95397
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway. |
-
Phytomedicine, 2022, 104:154283
|
|
S4013 |
Sodium Monofluorophosphate
|
Sodium Monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irreversibly inhibits phosphorylase phosphatase with Ki of 0.5 mM. |
|
|
S0918 |
Ginkgolic acid C17:1
|
Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
S6391 |
Sephin-1
|
Sephin-1 (NSC-65390) is a selective inhibitor of a holophosphatase, a small molecule that safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin-1 (NSC-65390) selectively bounds and inhibits the stress-induced PPP1R15A. |
|
|
E1191 |
GDC-1971
|
GDC-1971 (compound 199) is a SHP2 inhibitor. |
-
Nat Commun, 2024, 15(1):3805
|
|
S0744 |
Raphin1 acetate
|
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase with Kd of 0.033 μM. |
|
|
S5198 |
Sodium Etidronate
|
Sodium Etidronate (Didronel, EHDP, Etidronic acid) is a non-aminobisphosphonate that exhibits protein tyrosine phosphatase (PTP) inhibitory activity. |
|
|
E4016 |
Phenylarsine oxide
|
Phenylarsine oxide (Oxophenylarsine) is a membrane-permeable protein tyrosine phosphatase inhibitor with IC50 18 µM. It Stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle. |
|
|
S0302 |
F1063-0967
|
F1063-0967 is an inhibitor of Dual-specificity phosphatase 26 (DUSP26) with IC50 of 11.62 μM. |
|
|
E1207 |
Osunprotafib (ABBV-CLS-484)
|
Osunprotafib (ABBV-CLS-484) is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity. |
|
|
S0056 |
(E/Z)-BCI
|
(E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. |
|
|
E1165New |
JAB-3068
|
JAB-3068 (SHP2-IN-6) is a potent allosteric inhibitor of SHP2. JAB-3068 enhances the anti-tumor activity of CD8+ T cells and can be used in combination to address non-responsive tumors alongside PD-1/PD-L1 antibodies. |
|
|
E1171 |
SBI-425
|
SBI-425, a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor, effectively inhibits TNAP in the vasculature, improving cardiovascular parameters and survival. |
|
|
S6109 |
H-HoArg-OH
|
H-HoArg-OH (L-Homoarginine) is an organ-specific, uncompetitive inhibitor of serum "bone and liver" alkaline phosphatase. |
|
|
S3696 |
PTP Inhibitor I
|
PTP Inhibitor I is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor with Ki values of 43 and 42 μM for SHP-1(ΔSH2) and PTP1B, respectively.
|
|
|
E0758 |
Silydianin
|
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. |
|
|
S9703 |
BBP- 398 (IACS-13909)
|
BBP- 398 (IACS-13909) is a specific and potent allosteric inhibitor of SHP2 (Src homology 2 domain-containing phosphatase) that suppresses signaling through the MAPK pathway. |
-
J Neuroinflammation, 2024, 21(1):37
|
|
S0119 |
PTP1B-IN-2
|
PTP1B-IN-2 (MDK3465, Ptp1B-In-2, Compound P6) is a potent and selective protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 50 nM. PTP1B-IN-2 enhances insulin-mediated insulin receptor β (IRβ) phosphorylation and insulin-stimulated glucose uptake. |
|
|
S5788New |
Tacrolimus monohydrate
|
Tacrolimus monohydrate (Tacrolimus, FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP). This inhibition blocks calcium-dependent processes, including interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, and also has immunosuppressive, neuroregenerative and neuroprotective properties. |
|
|
S7383 |
(-)-p-Bromotetramisole Oxalate
|
(-)-p-Bromotetramisole Oxalate (L-p-Bromotetramisole Oxalate) is a potent and non-specific alkaline phosphatase inhibitor.
|
|
|
S2837 |
BCI
|
BCI ((E)-BCI, compound 1) is an allosteric dual specificity phosphatase (DUSP) inhibitor with EC50 of 13.3 μM and 8.0 μM in cells for DUSP6 and DUSP1, respectively. |
-
Cell Rep, 2023, 42(12):113568
|
|
S4451 |
NSC45586
|
NSC45586 is an inhibitor of PHLPP (Pleckstrin homology domain and leucine-rich repeat protein phosphatase), which is selective for PHLPP1 and PHLPP2. |
|
|
S0445 |
SC-43
|
SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity. |
|
|
S9913 |
PHPS1
|
PHPS1 (PTP Inhibitor V), a potent and cell-permeable inhibitor, is specific for Shp2 with Ki value of 0.73 μM.
|
|
|
E2692 |
L-Ascorbic acid 2-phosphate sesquimagnesium salt
|
L-Ascorbic acid 2-phosphate sesquimagnesium salt (2-Phospho-L-ascorbic acid magnesium), a long-acting vitamin C derivative that can stimulate collagen formation and expression, can be used as a culture medium supplement for the osteogenic differentiation of human adipose stem cells (hASCs), which increases alkaline phosphatase (ALP) activity and expression of runx2A in hASCs during the osteogenic differentiation. |
|
|
E1878New |
Bromoenol lactone
|
Bromoenol lactone((6E)-Bromoenol lactone) is a selective, irreversible, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of ≈7 μM. It prevents antigen-stimulated exocytosis in mast cells without hindering Ca2+ influx. |
|
|
S5441 |
1-Naphthyl phosphate potassium salt
|
1-Naphthyl phosphate potassium salt (α-Naphthyl acid phosphate monopotassium salt) is a non-specific phosphatase inhibitor which acts on acid, alkaline, and protein phosphatases. |
|
|
S5431 |
L-Homoarginine hydrochloride
|
L-Homoarginine is a specific inhibitor of liver-type alkaline phosphatase. |
|
|
E1780New |
Alexidine dihydrochloride
|
Alexidine dihydrochloride, a dibiguanide compound, is an effective and selective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1) with an IC50 of 1.08 μM in vitro. It has the potential to treat type II diabetes. |
|
|
E3790 |
Sambucus Adnata Extract
|
Sambucus Adnata Extract is drawed from Sambucus Adnata, which has shown significant protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity. |
|
|
E0140 |
PRL-3 Inhibitor (Compound 5e)
|
PRL-3 Inhibitor (Compound 5e) is a potent PRL-3 inhibitor with an IC50 of 0.9 μM.
|
|
|
E0956 |
MP07-66
|
MP07-66, a FTY720 analogue, is devoid of immunosuppressive effects and shows promising antitumor effects in chronic lymphocytic leukemia by disruption of the SET-PP2A complex leading to PP2A reactivation. |
|
|
S9829 |
BVT-948
|
BVT 948 is a irreversible, noncompetitive and cell-permeable protein tyrosine phosphatase(PTP) inhibitor with IC50s of 0.9 μM, 1.7 μM, 0.09 μM, 1.5 μM and 0.7 μM for PTP1B, TCPTP, SHP-2, LAR and YopH respectively. |
|
|
S0244 |
SPI-112
|
SPI-112 is a not cell permeable inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2, PTPN11) with IC50 of 1 μM in cell-free assay. |
|
|
S3284 |
Tracheloside
|
Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. Tracheloside significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. |
|
|
S2286 |
Cyclosporin A
|
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. |
- Cell Rep, 2024, S2211-1247(23)01591-7
- mSphere, 2024, 9(1):e0055423
- Food Chem Toxicol, 2024, 188:114665
|
|
S5003 |
Tacrolimus (FK506)
|
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. |
- Nat Immunol, 2024, 25(5):860-872
- Int J Antimicrob Agents, 2024, 63(5):107116
- Cell Commun Signal, 2024, 22(1):428
|
|
S8278 |
SHP099 HCl
|
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. |
- EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
- Pharmacol Res, 2024, 201:107096
- Biomed Pharmacother, 2024, 175:116590
|
|
S8718 |
RMC-4550
|
RMC-4550 is a potent SHP-2inhibitor with an IC50 of 1.55 nM and it has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels. |
- J Neuroinflammation, 2024, 21(1):37
- Cell Rep, 2023, 42(6):112570
- Oncogene, 2023, 42(20):1620-1633
|
|
S6388 |
SHP099
|
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. |
- MedComm (2020), 2024, 5(4):e527
- NPJ Precis Oncol, 2023, 7(1):136
- Front Immunol, 2023, 14:1260545
|
|
S1514 |
Cyclosporine
|
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation. |
- J Adv Res, 2024, S2090-1232(24)00499-5
- Cells, 2023, 12(23)2696
- Int J Mol Sci, 2023, 24(11)9708
|
|
S7573 |
GSK2830371
|
GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
|
- Cancer Res, 2022, canres.4145.2021
- Cancer Res, 2022, 82 (12): 2313–2326.
- iScience, 2022, 25(9):104892
|
|
S1949 |
Menadione (Vitamin K3)
|
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. |
- Med -N Y, 2022, S2666-6340-2200365-8
- Mol Cell, 2021, S1097-2765(21)00269-0
- DNA Repair (Amst), 2021, 105:103152
|
|
S4007 |
Pentamidine isethionate
|
Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein. |
- Nat Commun, 2022, 13(1):6323
- Biomed Chromatogr, 2022, e5519.
- Cell Prolif, 2020, 53(1):e12718
|
|
S3620 |
β-Glycerophosphate sodium salt hydrate
|
β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor. |
- Nat Commun, 2024, 15(1):2384
- Discov Oncol, 2024, 15(1):338
- Res Sq, 2023, rs.3.rs-2405644
|
|
S8182 |
NSC87877
|
NSC-87877 is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1/2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability/proliferation. |
- EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
- Inflammation, 2022, 10.1007/s10753-022-01762-6
- Oncotarget, 2020, 21;11(3):265-281
|
|
S7437 |
Sal003
|
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
- Front Pharmacol, 2023, 14:1095307
- bioRxiv, 2023, 2023.05.19.540602
- bioRxiv, 2023, 2023.05.19.540602
|
|
S8987 |
Batoprotafib(TNO155)
|
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. TNO155 has potential antineoplastic activity. |
- J Neuroinflammation, 2024, 21(1):37
- Pharmacol Res, 2024, 201:107096
- Mol Oncol, 2024, 10.1002/1878-0261.13725
|
|
S6570 |
TPI-1
|
TPI-1 (Tyrosine Phosphatase Inhibitor 1) is a potent inhibitor of SHP-1 with IC50 of 40 nM for recombinant SHP-1. TPI-1 exhibits anticancer activity. |
- Immunity, 2024, 57(2):287-302.e12
- Cell Rep Med, 2024, 5(1):101374
- EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1
|
|
S5452 |
Sanguinarine chloride
|
Sanguinarine, a plant alkaloid, is a potent and specific protein phosphatase (PP) 2C inhibitor. Sanguinarine chloride can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB. |
- Cell Rep, 2023, 42(3):112186
- Front Pharmacol, 2021, 12:638215
|
|
S1857 |
Etidronate
|
Etidronate is a non-aminobisphosphonate, show protein tyrosine phosphatase (PTP) inhibitory activity, used for the treatment of Paget's disease and the prevention of heterotopic ossification. |
- J Immunother Cancer, 2020, 8(2)e001037
|
|
S0528 |
Raphin1
|
Raphin1 is an orally bioavailable, selective inhibitor of R15B (PPP1R15B, a regulatory subunit of protein phosphatase 1). Raphin1 binds strongly to the R15B-PP1c holophosphatase with Kd of 33 nM. |
- Cell Rep, 2024, 43(8):114606
- Cell Stem Cell, 2022, 29(7):1119-1134.e7
|
|
S2435 |
Sodium stibogluconate
|
Sodium stibogluconate (SSG, Stibogluconate trisodium nonahydrate, Lenocta, VQD-001), a pentavalent antimony derivative, is a potent and selective inhibitor of protein tyrosine phosphatase (PTPase). Sodium stibogluconate inhibits 99% of Src homology 2 domain-containing phosphatase 1 (SHP-1) activity at 10 μg/ml and similar degrees of inhibition of SHP-2 and PTP1B requires 100 μg/ml. Sodium stibogluconate is a drug used in treatment of leishmaniasis. |
- Gastroenterology, 2024, S0016-5085(24)00062-3
- Biomed Chromatogr, 2022, e5519.
|
|
S5953 |
Menadione bisulfite sodium
|
Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
- Life Sci, 2020, 242:117159
|
|
S3678 |
PTP Inhibitor II
|
PTP Inhibitor II (NSC 129010, 4-(Bromoacetyl)anisole) is a cell-permeable protein tyrosine phosphatase (PTP) inhibitor that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with Ki value of 128 μM. |
- Fish Shellfish Immunol, 2020, 99:562-571
|
|
S7485 |
CCT007093
|
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM. |
- Oncogene, 2016, 35(42):5552-5564
|
|
S0136 |
KY-226
|
KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. |
- J Immunol, 2022, 209(9):1662-1673
|
|
S5595 |
3-Carene
|
3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. |
- Phytomedicine, 2021, 91:153707
|
|
S6777 |
NSC95397
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway. |
- Phytomedicine, 2022, 104:154283
|
|
S4013 |
Sodium Monofluorophosphate
|
Sodium Monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irreversibly inhibits phosphorylase phosphatase with Ki of 0.5 mM. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
S6391 |
Sephin-1
|
Sephin-1 (NSC-65390) is a selective inhibitor of a holophosphatase, a small molecule that safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin-1 (NSC-65390) selectively bounds and inhibits the stress-induced PPP1R15A. |
|
|
E1191 |
GDC-1971
|
GDC-1971 (compound 199) is a SHP2 inhibitor. |
- Nat Commun, 2024, 15(1):3805
|
|
S0744 |
Raphin1 acetate
|
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase with Kd of 0.033 μM. |
|
|
S5198 |
Sodium Etidronate
|
Sodium Etidronate (Didronel, EHDP, Etidronic acid) is a non-aminobisphosphonate that exhibits protein tyrosine phosphatase (PTP) inhibitory activity. |
|
|
E4016 |
Phenylarsine oxide
|
Phenylarsine oxide (Oxophenylarsine) is a membrane-permeable protein tyrosine phosphatase inhibitor with IC50 18 µM. It Stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle. |
|
|
S0302 |
F1063-0967
|
F1063-0967 is an inhibitor of Dual-specificity phosphatase 26 (DUSP26) with IC50 of 11.62 μM. |
|
|
E1207 |
Osunprotafib (ABBV-CLS-484)
|
Osunprotafib (ABBV-CLS-484) is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity. |
|
|
S0056 |
(E/Z)-BCI
|
(E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. |
|
|
E1165New |
JAB-3068
|
JAB-3068 (SHP2-IN-6) is a potent allosteric inhibitor of SHP2. JAB-3068 enhances the anti-tumor activity of CD8+ T cells and can be used in combination to address non-responsive tumors alongside PD-1/PD-L1 antibodies. |
|
|
E1171 |
SBI-425
|
SBI-425, a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor, effectively inhibits TNAP in the vasculature, improving cardiovascular parameters and survival. |
|
|
S6109 |
H-HoArg-OH
|
H-HoArg-OH (L-Homoarginine) is an organ-specific, uncompetitive inhibitor of serum "bone and liver" alkaline phosphatase. |
|
|
S3696 |
PTP Inhibitor I
|
PTP Inhibitor I is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor with Ki values of 43 and 42 μM for SHP-1(ΔSH2) and PTP1B, respectively.
|
|
|
E0758 |
Silydianin
|
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. |
|
|
S9703 |
BBP- 398 (IACS-13909)
|
BBP- 398 (IACS-13909) is a specific and potent allosteric inhibitor of SHP2 (Src homology 2 domain-containing phosphatase) that suppresses signaling through the MAPK pathway. |
- J Neuroinflammation, 2024, 21(1):37
|
|
S0119 |
PTP1B-IN-2
|
PTP1B-IN-2 (MDK3465, Ptp1B-In-2, Compound P6) is a potent and selective protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 50 nM. PTP1B-IN-2 enhances insulin-mediated insulin receptor β (IRβ) phosphorylation and insulin-stimulated glucose uptake. |
|
|
S5788New |
Tacrolimus monohydrate
|
Tacrolimus monohydrate (Tacrolimus, FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP). This inhibition blocks calcium-dependent processes, including interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, and also has immunosuppressive, neuroregenerative and neuroprotective properties. |
|
|
S7383 |
(-)-p-Bromotetramisole Oxalate
|
(-)-p-Bromotetramisole Oxalate (L-p-Bromotetramisole Oxalate) is a potent and non-specific alkaline phosphatase inhibitor.
|
|
|
S2837 |
BCI
|
BCI ((E)-BCI, compound 1) is an allosteric dual specificity phosphatase (DUSP) inhibitor with EC50 of 13.3 μM and 8.0 μM in cells for DUSP6 and DUSP1, respectively. |
- Cell Rep, 2023, 42(12):113568
|
|
S4451 |
NSC45586
|
NSC45586 is an inhibitor of PHLPP (Pleckstrin homology domain and leucine-rich repeat protein phosphatase), which is selective for PHLPP1 and PHLPP2. |
|
|
S9913 |
PHPS1
|
PHPS1 (PTP Inhibitor V), a potent and cell-permeable inhibitor, is specific for Shp2 with Ki value of 0.73 μM.
|
|
|
E1878New |
Bromoenol lactone
|
Bromoenol lactone((6E)-Bromoenol lactone) is a selective, irreversible, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of ≈7 μM. It prevents antigen-stimulated exocytosis in mast cells without hindering Ca2+ influx. |
|
|
S5441 |
1-Naphthyl phosphate potassium salt
|
1-Naphthyl phosphate potassium salt (α-Naphthyl acid phosphate monopotassium salt) is a non-specific phosphatase inhibitor which acts on acid, alkaline, and protein phosphatases. |
|
|
S5431 |
L-Homoarginine hydrochloride
|
L-Homoarginine is a specific inhibitor of liver-type alkaline phosphatase. |
|
|
E1780New |
Alexidine dihydrochloride
|
Alexidine dihydrochloride, a dibiguanide compound, is an effective and selective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1) with an IC50 of 1.08 μM in vitro. It has the potential to treat type II diabetes. |
|
|
E3790 |
Sambucus Adnata Extract
|
Sambucus Adnata Extract is drawed from Sambucus Adnata, which has shown significant protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity. |
|
|
E0140 |
PRL-3 Inhibitor (Compound 5e)
|
PRL-3 Inhibitor (Compound 5e) is a potent PRL-3 inhibitor with an IC50 of 0.9 μM.
|
|
|
S9829 |
BVT-948
|
BVT 948 is a irreversible, noncompetitive and cell-permeable protein tyrosine phosphatase(PTP) inhibitor with IC50s of 0.9 μM, 1.7 μM, 0.09 μM, 1.5 μM and 0.7 μM for PTP1B, TCPTP, SHP-2, LAR and YopH respectively. |
|
|
S0244 |
SPI-112
|
SPI-112 is a not cell permeable inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2, PTPN11) with IC50 of 1 μM in cell-free assay. |
|
|
S3284 |
Tracheloside
|
Tracheloside is a lignan glycoside isolated from seeds of Carthamus tinctorius with anti-estrogenic effects. Tracheloside significantly decreases the activity of alkaline phosphatase (AP) (an estrogen-inducible marker enzyme) with IC50 of 0.31 μg/ml. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. |
|
|