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1-NM-PP1, a cell-permeable PP1 analog, is a potent Src family kinases inhibitor with IC50s of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively [1] .
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1].
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1] .
3-IN-PP1 is a protein kinase D (PKD) inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC50 values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer [1].
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1(Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division [1] .
3BrB-PP1 is an ATP-competitive analog. 3BrB-PP1 can specifically inhibit the activity of protein kinase with mutations in the ATP-binding pocket (mutation of Thr97 within Sty1’s ATP-binding pocket) [1] .
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively [1].
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1(PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer [1].
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, respectively [1].
Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy [1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4(IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation [1] .
Cantharidic acid disodium is the hydrolysis product of the acid anhydride Cantharidin that induces apoptosis in various human cancer cells. Cantharidic acid disodium is a selective protein phosphatase 2 (PP2A) and PP1 inhibitor withIC50 values of 50 nM and 600 nM, respectively [1] .
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca( 2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis [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, autophagy 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] .
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4(IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation [1] .
Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A(IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4(IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation [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].
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].
α,α-Trehalose 6-phosphate (Standard) is the analytical standard of α,α-Trehalose 6-phosphate. This product is intended for research and analytical applications. α,α-Trehalose 6-phosphate (Tre6P) is an endogenous metabolite. α,α-Trehalose 6-phosphate is a 6-phosphate derivative of α,α′-trehalose. α,α-Trehalose 6-phosphate is rapidly converted to the pathway end product, α,α′-trehalose, through the action of Tre6P phosphatase (T6PP)[1].
α,α-Trehalose 6-phosphate (Tre6P) potassium is an endogenous metabolite. α,α-Trehalose 6-phosphate is a 6-phosphate derivative of α,α′-trehalose. α,α-Trehalose 6-phosphate is rapidly converted to the pathway end product, α,α′-trehalose, through the action of Tre6P phosphatase (T6PP) .
Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc.
Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action.
MCE supplies a unique collection of 132 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively [1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4(IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation [1] .
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively [1].
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1(PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer [1].
α,α-Trehalose 6-phosphate (Standard) is the analytical standard of α,α-Trehalose 6-phosphate. This product is intended for research and analytical applications. α,α-Trehalose 6-phosphate (Tre6P) is an endogenous metabolite. α,α-Trehalose 6-phosphate is a 6-phosphate derivative of α,α′-trehalose. α,α-Trehalose 6-phosphate is rapidly converted to the pathway end product, α,α′-trehalose, through the action of Tre6P phosphatase (T6PP)[1].
α,α-Trehalose 6-phosphate (Tre6P) potassium is an endogenous metabolite. α,α-Trehalose 6-phosphate is a 6-phosphate derivative of α,α′-trehalose. α,α-Trehalose 6-phosphate is rapidly converted to the pathway end product, α,α′-trehalose, through the action of Tre6P phosphatase (T6PP) .
PPP1CC protein is a multifunctional phosphatase that forms a specific holoenzyme with more than 200 regulatory proteins to dephosphorylate various biological targets. PPP1CC is critical for cell division and regulates glycogen metabolism, muscle contractility, and protein synthesis. PPP1CC Protein, Human (His) is the recombinant human-derived PPP1CC protein, expressed by E. coli , with N-6*His, C-6*His labeled tag. The total length of PPP1CC Protein, Human (His) is 323 a.a., with molecular weight of 30-40 kDa.
The multifunctional PL-PRO protein plays a critical role in viral RNA transcription and replication, providing the necessary proteases for multiprotein cleavage. It strategically blocks host translation by binding to the open head conformation of the 40S subunit, impeding ribosomal mRNA entry into the tunnel. PL-PRO Protein, 2019-nCoV (His) is the recombinant Virus-derived PL-PRO protein, expressed by E. coli , with N-6*His labeled tag. The total length of PL-PRO Protein, 2019-nCoV (His) is 312 a.a., .
The multifunctional SARS Plpro/papain-like protease protein utilizes essential proteases for multi-protein cleavage to strategically coordinate viral RNA transcription and replication. It blocks host translation by interacting with the 40S ribosomal subunit, causing endonucleolytic cleavage near the 5'UTR of host mRNAs, thereby targeting them for degradation. SARS Plpro/papain-like protease Protein (His-Avi) is the recombinant Virus-derived SARS Plpro/papain-like protease protein, expressed by E. coli , with N-His, N-Avi labeled tag. The total length of SARS Plpro/papain-like protease Protein (His-Avi) is 314 a.a., with molecular weight of ~38.6 kDa.
The multifunctional SARS-CoV-2 PP1ab protein is essential for viral RNA transcription and replication, utilizing proteases for multi-protein cleavage. It inhibits host translation by binding to the 40S subunit and blocks ribosomal mRNA entry channels, thereby hindering the antiviral response. SARS-CoV-2 PLpro Protein is the recombinant Virus-derived SARS-CoV-2 PLpro protein, expressed by E. coli , with tag free. The total length of SARS-CoV-2 PLpro Protein is 315 a.a., with molecular weight of ~34.0 kDa.
Protein Phosphatase 1G; Protein Phosphatase 1C; Protein Phosphatase 2C Isoform Gamma; PP2C-Gamma; Protein Phosphatase Magnesium-Dependent 1 Gamma; PPM1G; PPM1C
PP1MG Protein, a member of PPM family of serine/threonine phosphatases, has an important role in controlling cell cycle progression. PP1MG Proteinregulates the phosphorylation of SRSF3 in hepatocellular carcinoma (HCC) and contributes to the proliferation, invasion, and metastasis of HCC. PP1MG Protein forms a distinct holoenzyme complex with the PP2A regulatory subunit B56δ. B56δ‐PPM1G dephosphorylates α‐catenin at serine 641, which is necessary for the appropriate assembly of adherens junctions and the prevention of aberrant cell migration. PP1MG Protein, Human (His) is the recombinant human-derived PP1MG protein, expressed by E. coli , with C-6*His labeled tag. The total length of PP1MG Protein, Human (His) is 230 a.a., with molecular weight of ~30.0 kDa.
Protein Phosphatase 1 Regulatory Subunit 14A; 17 kDa PKC-Potentiated Inhibitory Protein of PP1; Protein Kinase C-Potentiated Inhibitor Protein of 17 kDa; CPI-17; PPP1R14A; CPI17; PPP1INL
The PPP1R14A protein is a key cellular regulator that effectively inhibits PPP1CA and exhibits significant activity amplification upon phosphorylation. This phosphorylation-induced transformation turns PPP1R14A into a dynamic molecular switch adept at regulating PPP1CA substrate phosphorylation. PPP1R14A Protein, Human (His) is the recombinant human-derived PPP1R14A protein, expressed by E. coli , with C-6*His labeled tag. The total length of PPP1R14A Protein, Human (His) is 147 a.a., with molecular weight of 23-26 kDa.
The PTP4A2 protein is an influential tyrosine phosphatase that stimulates G1 to S phase progression and contributes to cell cycle regulation. Notably, it promotes tumorigenesis, revealing its involvement in cancer development. PTP4A2 Protein, Human (GST) is the recombinant human-derived PTP4A2 protein, expressed by E. coli , with N-GST labeled tag. The total length of PTP4A2 Protein, Human (GST) is 166 a.a., with molecular weight of ~45.9 kDa.
The multifunctional SARS-CoV-2 PP1ab protein is essential for viral RNA transcription and replication, utilizing proteases for multi-protein cleavage. It inhibits host translation by binding to the 40S subunit and blocks ribosomal mRNA entry channels, thereby hindering the antiviral response. SARS-CoV-2 PP1ab Protein (His-MBP) is the recombinant Virus-derived SARS-CoV-2 PP1ab protein, expressed by E. coli , with C-6*His labeled tag. The total length of SARS-CoV-2 PP1ab Protein (His-MBP) is 601 a.a., with molecular weight of ~120.0 kDa.
The PTP4A2 protein is an influential tyrosine phosphatase that stimulates G1 to S phase progression and contributes to cell cycle regulation. Notably, it promotes tumorigenesis, revealing its involvement in cancer development. PTP4A2 Protein, Human (His) is the recombinant human-derived PTP4A2 protein, expressed by E. coli , with C-6*His labeled tag. The total length of PTP4A2 Protein, Human (His) is 167 a.a., with molecular weight of ~20 kDa.
