phosphatase

Inhibitory Selectivity

phosphatase Products

Catalog No. Information Product Use Citations Product Validations
S5003

Tacrolimus (FK506)

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.

S2286

Cyclosporin A

Cyclosporin A (Cyclosporine A) is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.

S1949

Menadione

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.

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.

S1514

Cyclosporine

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

S3245New

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.

S3284New

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.

S0918New

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.

S8987New

TNO155

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.

S0744New

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.

S2435New

Sodium stibogluconate

Sodium stibogluconate, 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.

S6570New

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.

S0528New

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.

S0302New

F1063-0967

F1063-0967 is an inhibitor of Dual-specificity phosphatase 26 (DUSP26) with IC50 of 11.62 μM.

S6777New

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.

S0119New

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.

S0136New

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.

S0056New

(E)-BCI

(E)-BCI (BCI, (E/Z)-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.

S4007

Pentamidine isethionate

Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.

S7437

Sal003

Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.

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.

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.

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.

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.

S3678

PTP Inhibitor II

PTP Inhibitor II 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.

S7485

CCT007093

CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.

S7383

(-)-p-Bromotetramisole Oxalate

(-)-p-Bromotetramisole Oxalate (L-p-Bromotetramisole Oxalate) is a potent and non-specific alkaline phosphatase inhibitor.

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.

S7573

GSK2830371

GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

S3670

Cefsulodin sodium

Cefsulodin (Sulcephalosporin) is a β-lactam antibiotic and inhibits mPTPB with the IC50 of 16 μM.

S3620

β-Glycerophosphate sodium salt hydrate

β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor.

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.

S5525

SodiuM Metatungstate

Sodium metatungstate (SMT) solution is an inorganic heavy liquid which is widely used in density fractionation. Sodium metatungstate (Sodium polyoxotungstates) is a potent and selective inhibitor of ecto-nucleoside triphosphate diphosphohydrolase (NTPDases) with Ki of 0.140 μM, 0.910 μM and 0.563 μM for NTPDase1, NTPDase2 and NTPDase3, respectively.

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.

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.

S5431

L-Homoarginine hydrochloride

L-Homoarginine is a specific inhibitor of liver-type alkaline phosphatase.

S9695New

iHAP1

iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells.

S0445New

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.

Catalog No. Information Product Use Citations Product Validations
S5003

Tacrolimus (FK506)

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.

S2286

Cyclosporin A

Cyclosporin A (Cyclosporine A) is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.

S1949

Menadione

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.

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.

S1514

Cyclosporine

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

S3245New

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.

S3284New

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.

S0918New

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.

S8987New

TNO155

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.

S0744New

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.

S2435New

Sodium stibogluconate

Sodium stibogluconate, 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.

S6570New

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.

S0528New

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.

S0302New

F1063-0967

F1063-0967 is an inhibitor of Dual-specificity phosphatase 26 (DUSP26) with IC50 of 11.62 μM.

S6777New

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.

S0119New

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.

S0136New

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.

S0056New

(E)-BCI

(E)-BCI (BCI, (E/Z)-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.

S4007

Pentamidine isethionate

Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.

S7437

Sal003

Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.

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.

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.

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.

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.

S3678

PTP Inhibitor II

PTP Inhibitor II 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.

S7485

CCT007093

CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.

S7383

(-)-p-Bromotetramisole Oxalate

(-)-p-Bromotetramisole Oxalate (L-p-Bromotetramisole Oxalate) is a potent and non-specific alkaline phosphatase inhibitor.

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.

S7573

GSK2830371

GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

S3670

Cefsulodin sodium

Cefsulodin (Sulcephalosporin) is a β-lactam antibiotic and inhibits mPTPB with the IC50 of 16 μM.

S3620

β-Glycerophosphate sodium salt hydrate

β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor.

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.

S5525

SodiuM Metatungstate

Sodium metatungstate (SMT) solution is an inorganic heavy liquid which is widely used in density fractionation. Sodium metatungstate (Sodium polyoxotungstates) is a potent and selective inhibitor of ecto-nucleoside triphosphate diphosphohydrolase (NTPDases) with Ki of 0.140 μM, 0.910 μM and 0.563 μM for NTPDase1, NTPDase2 and NTPDase3, respectively.

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.

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.

S5431

L-Homoarginine hydrochloride

L-Homoarginine is a specific inhibitor of liver-type alkaline phosphatase.

Catalog No. Information Product Use Citations Product Validations
S9695New

iHAP1

iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells.

Catalog No. Information Product Use Citations Product Validations
S0445New

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.

Tags: phosphatase inhibition | phosphatase inhibitor drugs | phosphatase activation | phosphatase targets | phosphatase inhibitor cancer | phosphatase assay | phosphatase signaling pathway | phosphatase inhibitor clinical trial | phosphatase inhibitor review