Eudebeiolide B is a compound that can be isolated from Salvia plebeia R. Br. Eudebeiolide B inhibits osteoclastogenesis by regulating RANKL-induced NF-κB, c-Fos and calcium signaling. Eudebeiolide B can be used for osteoclast-related diseases research[1].
3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC50 of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts[1][2].
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].
BN82002 is a synthetic inhibitor of CDC25 phophatases, with IC50s of 2.4-6.3 μM for recombinant CDC25 phosphatases.
PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases[1].
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].
Anticancer agent 144 (compound 444) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 144 can be used in cancer research[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].
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist[1][2].[3]..
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).
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively.[1][2] Okadaic acid eliminate metazoan symbionts/parasites by apoptosis[3].
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].
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
Methyl pseudolarate B, a natural diterpenoid, is a protein tyrosine phosphatase 1B (PTP1B) (Phosphatase) inhibitor with an IC50 value of 10.9 μM[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.
SHP394 is an orally efficacious protein tyrosine phosphatase SHP2 inhibitor with an IC50 of 23 nM[1].
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].
PHPS1 sodium 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].
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.
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity[1].
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].
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.