Phosphatase Inhibitor

TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).

Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity.

Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC₅₀ of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.

Luteolin 7-diglucuronide is the major flavonoid isolated from Aloysia triphylla and Verbena officinalis.

ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC₅₀ of 31.6 μM and a K_i of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC₅₀ of 5.32 μM.

JAB-3068 (SHP2-IN-6) is a potent SHP2 inhibitor, extracted from patent WO2017211303A1, compound 7, has an IC₅₀ of 25.8 nM.

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

CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy.

PTP1B-IN-1 (Compound 7a) is a small molecule inhibitor of PTP1B with an IC₅₀ value of 1.6 mM. It is often used as the mother core for derivatives of analogues.

trans-11-Eicosenoic acid is a fatty acid that inhibits the phosphatase activity of PtpA from Mycobacterium tuberculosis, with an IC₅₀ of 27.97 µM. trans-11-Eicosenoic acid is detected in the stems of alfalfa plants inoculated with Sinorhizobium meliloti LL11, but is absent in the stems of uninoculated alfalfa or the strain itself.

PP5-IN-1 is a competitive and selective serine/threonine protein phosphatase 5 (PP5) inhibitor with a K_i value of 244 nM. PP5-IN-1 induces extrinsic apoptosis (Apoptosis), disrupts the integrity of complex II, and activates Caspase 8. PP5-IN-1 can be used in research related to clear cell renal cell carcinoma.

BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC₅₀ values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.

PTP1B-IN-3 is a potent and orally active PTP1B inhibitor with IC₅₀s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 has antidiabetic and anticancer effects.

PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.

Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC₅₀ value for Slingshot 1 is 3 μM and the K_i value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2.

MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC₅₀ values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively. (A family of human MAPK-specific protein tyrosine phosphatases)

Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC₅₀: 2.61 µM; K_i: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc.

TNAP-IN-1 (Compound 1) is a selective tissue-nonspecific alkaline phosphatase (TNAP) inhibitor, with an IC₅₀ of 0.19 μM. TNAP-IN-1 can be used for the research of soft tissue calcification.

BAMB-4 (ITPKA-IN-C14) is a specific and membrane-permeable ITPKA inhibitor. BAMB-4 has high stability and membrane permeability and against the inositol-1,4,5-trisphosphate (InsP3) kinase activity of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with an IC₅₀ value of 20 μM. BAMB-4 can be used for the research of metastasis of lung cancer.

Diorcinol is a potent SHP1 inhibitor with an IC₅₀ value of 0.96 μM. Diorcinol can be isolated from Aspergillus sydowii. Diorcinol has good blood-brain barrier penetration and can be used for diabetes research.