Protein Ser/Thr Phosphatases
Protein Ser/Thr phosphatases, belonging to the superfamily of protein phosphatases, are a diverse group of phosphatases that catalyze dephosphorylation and specifically remove phosphate groups from phosphorylated Ser and Thr residues within their substrates. Protein Ser/Thr phosphatases are comprised of two distinct families of phosphatases, including PPP phosphatases and PPM (or PP2C-related) phosphatases, which are coded by two unrelated gene families but share remarkably similar architecture of catalytic domains. PPP family was initially divided into two classes, type-I phosphatases (PP1) and type-2 phosphatases (PP2) consisting of PP2A, PP2B and PP2C isoforms. Novel protein phosphatases, such as PP4, PP5, PP6 and PP7, are also included in PPP family. PPM family is comprised of a number of Mg2+-dependent phosphatases encoded by different genes, which are structurally related to PP2C.
- Cat.No. Product Name Information
- B1177 Nafamostat Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant.
- A8223 CID 2011756 CID-2011756 is a novel and potent inhibitor of protein kinase D1 (PKD1), one of three PKD isoforms of a novel family of serine/threonine kinases involved in cell proliferation, survival, invasion and protein transport, with a value of 50% inhibition concentration IC50 of 3.2 μM in vitro.
- A4544 NSC 87877 IC50: NSC-87877 potently inhibited Shp2 with an IC50 of 0.318 ± 0.049 μM. NSC-87877 seemed to have no selectivity between human Shp2 and Shp1 (IC50 0.355 ± 0.073μM).
- A4543 BVT 948 PTPs inhibitor
- A4542 Alexidine dihydrochloride Selective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1) (IC50 = 1.08 μM in vitro). Stimulates increased insulin secretion by β-cells in rat pancreatic islets. Displays antitcancer properties in FaDu cells.
- A4541 Sal 003 Cell-permeable inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Analog of salubrinal with improved aqueous solubility. Shown to prevent the induction of hippocampal long-term potentiation (LTP) and memory formation (LTM) in mice.
- A4540 Okadaic acid Potent inhibitor of protein phosphatase 1 (IC50 = 3 nM) and protein phosphatase 2A (IC50 = 0.2-1 nM). Displays > 100,000,000-fold selectivity over PP2B and PP2C. Tumor promotor. Shown to activate atypical protein kinase C in adipocytes.
- A4539 NFAT Inhibitor Selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Does not disrupt other calcineurin-dependent pathways. Inhibits NFAT activation and NFAT-dependent expression of endogenous cytokine genes in T cells.
- A4538 INCA-6 INCA-6 is a selective inhibitor of transcription factor NFAT with Kd value of 0.8 mM in vitro.
- A4537 Fumonisin B1 Mycotoxin produced by Fusarium moniliforme. Potently inhibits sphingosine N-acyltransferase (ceramide synthase), causing an accumulation of sphingoid bases (IC50 ~ 75 nM). Also inhibits protein phosphatases; IC50 values are 80, 300, 400, 500 and 3000 μM for PP5, PP2Cα, PP2A, PP1γ2 and PP2B respectively.