PTP-family 选择性抑制剂 | 激活剂 | 激动剂

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.

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.

IACS-13909

IACS-13909 is a specific and potent allosteric inhibitor of SHP2 (Src homology 2 domain-containing phosphatase) that suppresses signaling through the MAPK pathway.

Sodium Etidronate

Sodium Etidronate (Didronel, EHDP, Etidronic acid) is a non-aminobisphosphonate that exhibits protein tyrosine phosphatase (PTP) inhibitory activity.

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.

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.

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.

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.

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.

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.

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.

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.

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.

PHPS1

PHPS1 (PTP Inhibitor V), a potent and cell-permeable inhibitor, is specific for Shp2 with Ki value of 0.73 μM.

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.

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.

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.

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.

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.

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.

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.

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.