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Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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 [2].
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 [2] .
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 .
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 [2] .
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
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 [2].
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis [2] .
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 .
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 .
Cyclosporin A (Standard) is the analytical standard of Cyclosporin A. This product is intended for research and analytical applications. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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 .
PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tau protein-related neurodegenerative diseases (Alzheimer's disease) [2].
AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma [2] .
NSC45586 sodium is an inhibitor of PHLPP. NSC45586 sodium targets the PP2C phosphatase domains of PHLPP1 and PHLPP2, blocks the phosphatase activity of PHLPP, increases the expression level of FOXO1 in the nucleus, and reduces the protein expression of PHLPP1. NSC45586 sodium activates the AKT survival signaling pathway, enhances IGF-1-induced AKT activation, and inhibits the phosphorylation of AKT/ERK under basal conditions. NSC45586 sodium reduces staurosporine-induced neuronal death, preserves notochord cell morphology and KRT19 expression, inhibits cell apoptosis (apoptosis), improves the viability and proliferation of nucleus pulposus cells, upregulates the expression of ACAN/SOX9, and downregulates the expression of MMP13. NSC45586 sodium binds tightly to bovine serum albumin (bovine serum albumin), and exerts a more significant effect on nucleus pulposus in male individuals. NSC45586 sodium can be used in studies related to global cerebral ischemia and intervertebral disc degeneration [2].
PROTAC Her3 Degrader-8 (Compound PP2) is a Her3 PROTAC degrader. PROTAC Her3 Degrader-8 promotes the ubiquitination and degradation of Her3. PROTAC Her3 Degrader-8 can be used in the study of lung adenocarcinoma and ovarian cancer (Pink: Her3 ligand (HY-107450); Blue: E3 ligase ligand (HY-170861); Black: linker (HY-Y1760)) .
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 [2].
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 [2].
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 [2] .
AS6 (3'-Hexylsulfanylabscisic acid) is a PYL antagonist with a Kd value of 0.48 μM for Arabidopsis PYL5. AS6 binds to PYL proteins, and its S-hexyl chain blocks PP2C binding via steric hindrance. AS6 alleviates the inhibitory effect of ABA on seed germination in Arabidopsis and lettuce .
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 Bleomycin hydrochloride (HY-17565A)-treated animals. ATUX-1215 can slow the progression of lung fibrosis .
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.
Fostriecin (sodium) (compound 1, CI-920) is an antibiotic with a cytotoxic activity. Fostriecin (sodium) is also an inhibitor of protein phosphatase including PP4 (IC50= 3 nM)and PP2 (IC50=1.5 nM) .
Antabactin is an ABA receptor antagonist. Antabactin blocks the ABA receptor-PP2C interaction thereby reducing ABA signaling. Antabactin restores germination of thermoinhibited lettuce .
MP07-66, a FTY720 analogue, is devoid of immunosuppressive effects and shows promising antitumor effects in chronic lymphocytic leukemia by disruption of the SET-PP2A complex leading to PP2A reactivation .
PPA24 is a PP2A activator with a KD of 8.465 μM for PP2ACα. PPA24 induces cancer cell death via apoptosis. PP2ACα induces ROS generation and decreases the level of c-Myc expression. PPA24 can be used to study colorectal cancer (CRC), Folinic acid (HY-17556), 5-Fluorouracil (HY-90006), and Oxaliplatin (HY-17371) (FOLFOX)-resistant CRC, and melanoma cancer [2] .
PP2 (Standard) is the analytical standard of PP2. This product is intended for research and analytical applications. PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
PPM1A-IN-1 (Compound IV-4) is an inhibitor for PP2C Ser/Thr phosphatase protein phosphatase Mg2+/Mn2+-dependent 1A. PPM1A-IN-1 exhibits antibacterial activity against Mycobacterium tuberculosis .
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 .
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.
PP2 Analog (compound 3) is a ATP-competitive Src family kinases inhibitor with the IC50 values of 0.22, 0.15, 2.68, and 7 aganist of lck (64-509), src , kdr, and tie-2 .
HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases .
Ceramide (Egg) (Ceramide (Egg, Chicken)) is a ceramide from chicken. Ceramide (Egg) is a sphingomyelin signaling pathway second messenger.Ceramide (Egg) activates PP2A, JNK, p38 MAPK, CAPK, ceramide-activated protein phosphatase, Vav, PKCζ, and SAPK/JNK cascade.Ceramide (Egg) downregulates or inhibits AKT, survivin, CDK2, mTOR, and FLIP.Ceramide (Egg) mediates apoptosis, autophagy, cell cycle arrest, mitochondrial dysfunction, redox state shifts, and ROS generation.Ceramide (Egg) can be used for the research of cancer and neurological disease[2] .
Anticancer agent 7 (Example 5) modulates PP2A, and induces FOXOl transcription factor translocation to the nucleus. Anticancer agent 7 inhibits the proliferation of H1650 lung cancer cell with an IC50 of 5 μM .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM [2]. Cyclosporin A also inhibits CD11a/CD18 adhesion .
NSC45586 is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 can activate AKT in neurons .
D-erythro-Sphingosine (Standard) is the analytical standard of D-erythro-Sphingosine. This product is intended for research and analytical applications. 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].
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
Cytostatin is an effective and selective protein phosphatase 2A (PP2A) inhibitor with an IC50 value of 210 nM. Cytostatin exhibits anti-metastatic properties, good antitumor activity, and can induce apoptosis. Cytostatin can also prevent the adhesion of B16 melanoma cells to components of the extracellular matrix (laminin and collagen). Cytostatin belongs to the family of natural product fosriecin [2] .
1,4-Dimethylnaphthalen is a non-competitive potato tuber sprouting inhibitor. 1,4-Dimethylnaphthalen blocks cell cycle progression (G1/S arrest) by inducing PP2A phosphatase and oxygen metabolism-related genes. 1,4-Dimethylnaphthalen is promising for research of fungistatic activity during potato storage and sprout control under abiotic stress [2].
TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research .
Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC50 = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC50 value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability. [2].
Cyclosporin A-d12 (Cyclosporine A-d12) is deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
MASTL kinase is a master regulator of mitosis, essential for ensuring that mitotic substrate phosphorylation is correctly maintained. It achieves this through the phosphorylation of alpha-endosulfine and subsequent inhibition of the tumor suppressor PP2A-B55 phosphatase. MASTL Recombinant Human Active Protein Kinase is a recombinant MASTL protein that can be used to study MASTL-related functions .
Oscillamide C (Compound 2), a ureido-containing cyclic peptide, is a Protein phosphatase 1 (PP1) and Protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.90 and 1.33 μM for PP1 and PP2A, respectively. Oscillamide C can be isolated from the cyanobacteria Planktothrix agardhii and P. rubescens. Oscillamide C can be used for cancers research .
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM [2]. Cyclosporin A also inhibits CD11a/CD18 adhesion .
Voclosporin (Standard) is the analytical standard of Voclosporin. This product is intended for research and analytical applications. Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor .
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 .
ATUX-8385 is a potent PP2A activator. ATUX-8385 binds to PR65 subunit. ATUX-8385 has the potential for the research of cancers and chronic conditions such as Alzheimer’s disease and chronic obstructive pulmonary disease .
FTY720-Mitoxy is a fingolimod hydrochloride (HY-12005) derivative with neuroprotective and PP2A activating activities. FTY720-Mitoxy has the property of targeting mitochondria. In addition, FTY720-Mitoxy protects neurons by reducing inflammatory responses and is used in the study of neurodegenerative diseases such as Parkinson's disease .
Cantharidic acid is a selective inhibitor for protein phosphatase 2(PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
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.
ITH12711 is a PP2A ligand. ITH12711 is able to cross the blood-brain barrier (BBB). ITH12711 exerts neuroprotection via restoration of PP2A-phosphatase activity .
Fenvalerate-d5 is the deuterium labeled Fenvalerate. 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 .
Fenvalerate (Standard) is the analytical standard of Fenvalerate. This product is intended for research and analytical applications. 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 .
Endothall (Standard) is the analytical standard of Endothall. This product is intended for research and analytical applications. 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 .
Oscillamide C TFA (Compound 2), a ureido-containing cyclic peptide, is a Protein phosphatase 1 (PP1) and Protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.90 and 1.33 μM for PP1 and PP2A, respectively. Oscillamide C TFA can be isolated from the cyanobacteria Planktothrix agardhii and P. rubescens. Oscillamide C TFA can be used for cancers research .
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 [2] .
D-erythro-Sphingosine-13C2,d2 is a deuterated 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 [2] .
(1S,2S,3R)-DT-061 is an enantiomer of DT-061 (HY-112929). DT-061 is an orally active activator of protein phosphatase 2A (PP2A). (1S,2S,3R)-DT-061 can be used as a negative control in the research of KRAS-mutant and MYC-driven lung cancer tumorigenesis .
CaMKP inhibitor sodium (compound 5) is an inhibitor of Ca 2+/neutral protein-dependent protein concentration (CaMKP) and its nuclear type (CaMKP-N) (IC50: 6.4 μM, CaMKP; 6.6 μM, CaMKP-N). CaMKP is one type of Ser/Thr protein, which can be passed through to remove the oxidized oxidized protein (CaMK). CaMKP inhibitor sodium inhibits CaMKP mediated phospho-CaMKI hydrolysis, unaffectes protein phosphoric acid 2C (PP2C) and calcineurin (CaN) .
MKI-2 is a selective MASTL inhibitor with an IC50 of 37.44 nM. MKI-2 induces mitotic catastrophe resulting from the modulation of the MASTL-PP2A axis in breast cancer cells. MKI-2 reduces phospho-ENSA, total, phospho-c-Myc levels. MKI-2 inhibts cancer cells proliferation, migration and induces DNA damage. MKI-2 inhibits germinal vesicle breakdown in mouse oocytes. MKI-2 can be used for the research of cancer, such as breast cancer .
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 174 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.
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research .
Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC50 = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC50 value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability. [2].
Oscillamide C (Compound 2), a ureido-containing cyclic peptide, is a Protein phosphatase 1 (PP1) and Protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.90 and 1.33 μM for PP1 and PP2A, respectively. Oscillamide C can be isolated from the cyanobacteria Planktothrix agardhii and P. rubescens. Oscillamide C can be used for cancers research .
Oscillamide C TFA (Compound 2), a ureido-containing cyclic peptide, is a Protein phosphatase 1 (PP1) and Protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.90 and 1.33 μM for PP1 and PP2A, respectively. Oscillamide C TFA can be isolated from the cyanobacteria Planktothrix agardhii and P. rubescens. Oscillamide C TFA can be used for cancers research .
Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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 [2].
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 [2] .
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis [2] .
Cyclosporin A (Standard) is the analytical standard of Cyclosporin A. This product is intended for research and analytical applications. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
Fostriecin (sodium) (compound 1, CI-920) is an antibiotic with a cytotoxic activity. Fostriecin (sodium) is also an inhibitor of protein phosphatase including PP4 (IC50= 3 nM)and PP2 (IC50=1.5 nM) .
D-erythro-Sphingosine (Standard) is the analytical standard of D-erythro-Sphingosine. This product is intended for research and analytical applications. 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].
Cytostatin is an effective and selective protein phosphatase 2A (PP2A) inhibitor with an IC50 value of 210 nM. Cytostatin exhibits anti-metastatic properties, good antitumor activity, and can induce apoptosis. Cytostatin can also prevent the adhesion of B16 melanoma cells to components of the extracellular matrix (laminin and collagen). Cytostatin belongs to the family of natural product fosriecin [2] .
1,4-Dimethylnaphthalen is a non-competitive potato tuber sprouting inhibitor. 1,4-Dimethylnaphthalen blocks cell cycle progression (G1/S arrest) by inducing PP2A phosphatase and oxygen metabolism-related genes. 1,4-Dimethylnaphthalen is promising for research of fungistatic activity during potato storage and sprout control under abiotic stress [2].
The ILKAP/PP2C delta protein is a key phosphatase that potentially regulates cell cycle progression by dephosphorylating substrates essential for proliferation. It selectively binds to ILK and regulates cell adhesion and growth factor signaling. ILKAP/PP2C delta Protein, Human (HEK293, His) is the recombinant human-derived ILKAP/PP2C delta protein, expressed by HEK293 , with C-His labeled tag.
PPM1A is a multifunctional enzyme whose enzymatic activity exhibits broad specificity. It acts as a negative regulator of TGF-β signaling by dephosphorylating SMAD2 and SMAD3, leading to their dissociation from SMAD4, nuclear export of SMAD, and termination of TGF-β-mediated signaling. PPM1A Protein, Mouse (His) is the recombinant mouse-derived PPM1A protein, expressed by E. coli , with C-His labeled tag.
PPM1A is a multifunctional enzyme that negatively regulates multiple signaling pathways. It significantly attenuates TGF-β signaling by dephosphorylating SMAD2 and SMAD3, leading to their dissociation from SMAD4, nuclear export, and signal termination. PPM1A Protein, Human (His) is the recombinant human-derived PPM1A protein, expressed by E. coli , with C-6*His labeled tag.
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.
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 [2] .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM [2]. Cyclosporin A also inhibits CD11a/CD18 adhesion .
Cyclosporin A-d12 (Cyclosporine A-d12) is deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM [2]. Cyclosporin A also inhibits CD11a/CD18 adhesion .
Fenvalerate-d5 is the deuterium labeled Fenvalerate. 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 .
D-erythro-Sphingosine-13C2,d2 is a deuterated 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 [2] .
Phospho-PP2A alpha (Tyr307) Antibody (YA2856) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospho-PP2A alpha (Tyr307).
Alpha isoform serine threonine protein phosphatase pp1alpha 1 catalytic subunit; Catalytic subunit; pp1A; pp1A_HUMAN; pp1alpha; pp2C ALPHA; pp2CA; ppp1ca; Protein Phosphatase 2C Alpha Isoform; Serine threonine protein phosphatase pp1 alpha catalytic subunit; Serine threonine protein phosphatase pp1 alpha catalytic subunit protein phosphatase 1; Serine/threonine-protein phosphatase pp1-alpha catalytic subunit.
WB, IHC-P, IP
Human, Mouse, Rat
Phospho-PPP1CA (Thr320) Antibody (YA9841) is a Rabbit-derived and non-conjugated IgG Recombinant, Monoclonal antibody, targeting to Phospho-PPP1CA (Thr320).
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.
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.
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.
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 .
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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