(Rac)-RK-682, a racemate of RK-682, is a protein tyrosine phosphatases (PTPases) inhibitor. (Rac)-RK-682 inhibits protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B) with IC50s of 8.6 μM, 12.4 μM, and 0.7 μM, respectively[1].
3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
Lumigen APS-5 is a substrate of alkaline phosphatase (ALP). Lumigen APS-5 can be used to assess the activity of alkaline phosphatase (ALP)[1].
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes[1].
DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect[1][2][3].
PTPN2/1-IN-2 is a PTPN2/1 antagonist that can be used in various tumor research[1].
Aloe-emodin-8-O-β-D-glucopyranoside, a compound isolated from Saussrurea lappa, is a moderate inhibitor of human protein tyrosine phosphatase 1B (hPTP1B) with an IC50 of 26.6 μM[1].
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively[1].
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation.
Limocitrin is a natural product that can be isolated from the buds of P. acerifolia and P. orientalis. Limocitrin suppresses estradiol-dependent proliferation of MCF7 cells weakly but estradiol-induced AlkP (alkaline phosphatase) expression only marginally[1].
PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases[1].
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease[1].
PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases[1].
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression[1].
NC1 is a novel highly active allosteric inhibitor of protein tyrosine phosphatase, non-receptor type 22 (PTPN22) which is a lymphoid-specific tyrosine phosphatase (LYP).
Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively[1][2].
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies[1].
2-Hydroxymethyl-3-hydroxyanthraquinone is an antiosteoporotic compound that inhibits osteoclastic tartrate-resistant acid phosphatase (TRAP) activity[1].
GS-493 is a novel potent, selective SHP2 inhibitor with IC50 of 71±15 nM in enzyme assay; displays 29- and 45-fold selectivity against related SHP1 and PTP1B; blocks HGF-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells, and inhibits cell colony formation in the NSCLC cell line LXFA 526L in soft agar; inhibits tumor growth in murine xenograft model.
SHP2-IN-7 is an SHP2 inhibitor extracted from patent WO2018013597[1].
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss[1][2][3][4][5].
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity[1].
Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes[1][2].
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis[1].
MY10 is a small-molecule inhibitor of RPTPβ/ζ (PTPRZ1) with IC50 of 0.1 uM, significantly increases the phosphorylation of key tyrosine residues of RPTPβ/ζ substrates involved in neuronal survival and differentiation; blocks ethanol conditioned place preference, shows limited effects on ethanol-induced ataxia, and potentiates the sedative effects of ethanol in mice; increases levels of phosphorylated ALK and TrkA in neuroblastoma cells, modulates signaling pathways activated by alcohol.
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus[1][2][3].
KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity; shows no effects on adipocyte differentiation in rodent preadipocytes at 10 uM, bot not the PPARγ agonist pioglitazone; increases the phosphorylated insulin receptor (pIR) produced by insulin in human hepatoma-derived cells (HepG2) at 0.310 uM, significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain in db/db mice, exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling.
Sephin 1 (NSC 65390) is a selective inhibitor of PPP1R15A that disrupts the PPP1R15A-PP1c complex but spares the related PPP1R15B-PP1c complex; prolongs eIF2α phosphorylation after stress, attenuates the expression of stress genes such as CHOP, and protects cells from cytotoxic ER stress; lacks any measurable α2-adrenergic agonist activity in a cell-based assay, in contrast to Guanabenz; safely prevents the motor, morphological, and molecular defects in mice.
PTP1B-IN-22, a ZINC02765569 derivative, is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor. PTP1B-IN-22 has PTP1B inhibition and glucose uptake in skeletal muscle L6 myotubes[1].