PP2A inhibitor

By Targets:	Akt (3) Antibiotic (1) Apoptosis (8) Endogenous Metabolite (1) Phosphatase (15) PKC (1)
By Research Areas:	Cancer (18) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	Alkynes (3)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-113976A

Endothall Endothal	Phosphatase
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 .

HY-18983

Calyculin A Maximum Cited Publications 13 Publications Verification (-)-Calyculin A	Phosphatase	Cancer
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 .

HY-139296

PP2A Cancerous-IN-1	Akt	Cancer
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-W328402

(Rac)-LB-100

Others Cancer

(Rac)-LB-100 is the racemate of LB-100. LB-100 is a protein phosphatase 2A (PP2A) inhibitor .

(Rac)-LB-100	Others	Cancer
(Rac)-LB-100 is the racemate of LB-100. LB-100 is a protein phosphatase 2A (PP2A) inhibitor .

HY-126730

Rubratoxin A	Phosphatase	Cancer
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC₅₀ of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .

HY-P0219

Microcystin-LA	Phosphatase	Cancer
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 .

HY-137552

MKI-1 MASTL Kinase inhibitor-1	Others	Cancer
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC₅₀ of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer .

HY-18597

LB-100

5+ Cited Publications

Phosphatase Cancer

LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC₅₀ of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells .

LB-100 5+ Cited Publications	Phosphatase	Cancer
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC₅₀ of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells .

HY-113612

Cytostatin	Phosphatase Apoptosis	Cancer
Cytostatin is a potent and selective inhibitor of *PP₂A* with promising antitumor activity. Cytostatin is also an inhibitor of cell adhesion to extracellular matrix and induces cell apoptosis. Cytostatin belongs to the fostriecin family of natural products .

HY-12833

AMZ30 1 Publications Verification	Others	Others
AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1; IC50=600 nM); selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells.

HY-137135A

Cantharidic acid disodium	Phosphatase Apoptosis	Cancer
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 .

HY-101047

D-erythro-Sphingosine 2 Publications Verification 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 .

HY-N10223

Phostriecin	Antibiotic Phosphatase	Infection Inflammation/Immunology Cancer
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 .

HY-147071

1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine DAPE	Others	Metabolic Disease
1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine (DAPE) is a phospholipid phosphatidylethanolamine. Unlike other phospholipid phosphatidylethanolamines, 1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine has no significant effect on protein phosphatase PP2A activity and does not inhibit insulin-stimulated GLUT4 translocation .

HY-101047S

D-erythro-Sphingosine-d7 Erythrosphingosine-d₇; erythro-C18-Sphingosine-d₇; trans-4-Sphingenine-d₇	PKC Phosphatase Endogenous Metabolite	Cancer
D-erythro-Sphingosine-d₇ is the deuterium labeled D-erythro-Sphingosine. 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[1][2][3][4].

HY-113612A

Cytostatin sodium	Apoptosis Phosphatase	Cancer
Cytostatin sodium is an effective and selective protein phosphatase 2A (PP2A) inhibitor with an IC50 value of 210 nM. Cytostatin sodium exhibits anti-metastatic properties, good antitumor activity, and can induce apoptosis. Cytostatin sodium can also prevent the adhesion of B16 melanoma cells to components of the extracellular matrix (laminin and collagen). Cytostatin sodium belongs to the family of natural product fosriecin .

HY-101180

C2 Ceramide 1 Publications Verification Ceramide 2
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 .

HY-N6785

Okadaic acid 5+ Cited Publications	Phosphatase Apoptosis	Neurological Disease Cancer
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 .

HY-N6785A

Okadaic acid sodium	Phosphatase Apoptosis	Neurological Disease Cancer
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 .

HY-115760

Okadaic acid ammonium salt	Phosphatase	Neurological Disease Cancer
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 .

HY-135699

TD52 1 Publications Verification	Apoptosis Phosphatase Akt	Cancer
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-135699A

TD52 dihydrochloride 1 Publications Verification	Akt Phosphatase Apoptosis	Cancer
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-156420

ATUX-1215	Others	Others
ATUX-1215 is an activator of protein phosphatase 2A (PP2A). ATUX-1215 reduced the phosphorylation of ERK, p38, JNK, and Akt and the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals. ATUX-1215 can slow the progression of lung fibrosis .

HY-N4317

Ethoxysanguinarine 1 Publications Verification	Apoptosis	Cancer
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine is an inhibitor of protein phosphatase 2A (CIP2A). Ethoxysanguinarine induces cell apoptosis and inhibits colorectal cancer cells growth .

Cat. No.	Product Name

HY-L081

Phosphatase Inhibitor Library	132 compounds
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.

Phosphatase Inhibitor Library

132 compounds

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.

Cat. No.	Product Name	Target	Research Area

HY-P0219

Microcystin-LA	Phosphatase	Cancer
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 .

Cat. No.	Product Name

HY-K0021

Phosphatase Inhibitor Cocktail I 350+ Cited Publications
Phosphatase Inhibitor Cocktail I effectively inhibits alkaline phosphatases and serine/threonine protein phosphatases such as PP1 and PP2A.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6785

Okadaic acid Maximum Cited Publications 7 Publications Verification	Structural Classification Animals Ketones, Aldehydes, Acids Marine natural products Source classification Other marine organisms	Phosphatase Apoptosis
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 .

HY-N4317

Ethoxysanguinarine 1 Publications Verification	Alkaloids Classification of Application Fields Source classification Quinoline Alkaloids Macleaya cordata (Willd.) R. Br. Plants Disease Research Fields Papaveraceae Cancer	Apoptosis
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine is an inhibitor of protein phosphatase 2A (CIP2A). Ethoxysanguinarine induces cell apoptosis and inhibits colorectal cancer cells growth .

HY-P0219

Microcystin-LA	Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields Cancer	Phosphatase
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 .

HY-113612

Cytostatin	Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields Cancer	Phosphatase Apoptosis
Cytostatin is a potent and selective inhibitor of *PP₂A* with promising antitumor activity. Cytostatin is also an inhibitor of cell adhesion to extracellular matrix and induces cell apoptosis. Cytostatin belongs to the fostriecin family of natural products .

HY-N10223

Phostriecin	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Inflammation/Immunology Disease Research Fields Other Antibiotics	Antibiotic Phosphatase
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 .

Cat. No.	Product Name	Chemical Structure

HY-101047S

D-erythro-Sphingosine-d7
D-erythro-Sphingosine-d₇ is the deuterium labeled D-erythro-Sphingosine. 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[1][2][3][4].

Cat. No.	Product Name		Classification

HY-135699

TD52 1 Publications Verification		Alkynes
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-135699A

TD52 dihydrochloride 1 Publications Verification		Alkynes
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-139296

PP2A Cancerous-IN-1		Alkynes
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Screening Libraries

Peptides

MCE Kits

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

PP2A inhibitor

Inhibitors & Agonists

Screening Libraries

Peptides

MCE Kits

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products