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Phosphatase inhibitors act on protein, lipid and inositol phosphatases that hydrolyze phosphate esters. A 2004 survey of the human genome counted 107 genes for protein tyrosine phosphatases (PTPs). Serine/threonine phosphatases such as protein phosphatases 1 and 2A (PP1, PP2A) reverse many kinase-driven signals. Calyculin A, reported in 1989 as an inhibitor of protein phosphatase activity, blocks both PP1 and PP2A. LB-100 targets PP2A, tautomycetin prefers PP1, and sodium orthovanadate inhibits PTPs broadly and is a common lysis buffer additive. Among lipid and inositol phosphatases, 3AC inhibits Src homology 2 (SH2) domain-containing inositol 5-phosphatase 1 (SHIP1), and L-690330 targets inositol monophosphatase.
Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
NSC 95397 is a selective and effective dual-specificity, quinone-based phosphatase inhibitor.
LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Synonyms: (-)-Calyculin A
Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM.
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively.
Synonyms: Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
Synonyms: NSC 65390; Sephin-1; IFB-088
Sephin1 is a selective inhibitor of stress-induced PPP1R15A and targets disease associated with accumulation of misfolded protein.
Synonyms: 3α-Aminocholestane
3AC is a cell-permeable, selective inhibitor of SHIP1 polyphosphatase activity toward PIP3 (IC50 = 10 μM), but has no effect on SHIP2 or PTEN activity on PIP3.
Tautomycetin induces apoptosis by inactivating Akt through a PP1-independent signaling pathway in human breast cancer cells.
Synonyms: L-p-Bromotetramisole Oxalate
(-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor.
CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1.
Synonyms: Macrofusine; Macrofusin
Fumonisin B1 is a fungal metabolite produced by Fusarium moniliforme, that has been shown to inhibit protein serine/threonine phosphatases (PP1, PP2A, PP2B, PP2C, and PP5/T/K/H), and is most effective with PP5.
CPDA is a novel potent SHIP2 inhibitor that can effectively ameliorate insulin resistance in 3T3-L1 adipocytes.
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
Synonyms: Ribozinoindole-1
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
NSC117079 is a novel pan-PHLPP inhibitors (selective for PHLPP1 and PHLPP2).
F1063-0967 is a novel inhibitor of dual-specificity phosphatase 26 (DUSP26), inducing apoptosis in IMR-32 cell line.
AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1) with IC50 value of 600 nM.
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
Synonyms: Flavylium
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity.
Synonyms: DT1154
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A.
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B).
