Search Result
Results for "
Acid phosphatase Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-D0852
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Phosphatase
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Cancer
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Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
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-
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- HY-115759
-
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Others
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Metabolic Disease
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N-Octylmaleimide is an alkylmaleimide, which can inhibit rat liver glucose 6-phosphatase .
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-
-
- HY-148001
-
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Phosphatase
Dopamine β-hydroxylase
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Others
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EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity .
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-
-
- HY-149492
-
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Phosphatase
Fungal
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Infection
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Phosphatase-IN-1 (compound II-8), a propranolol (HY-B0573B) derivative, is a phosphatidate phosphatase (Pah) inhibitor. Phosphatase-IN-1 can binds to MoPah1, with an affinity constant of 19.8 μM. Phosphatase-IN-1 inhibits growth of plant pathogens and shows anti-fungal ability. Phosphatase-IN-1 is not toxic to rice seedlings and wheat heads .
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-
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- HY-16443
-
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Others
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Metabolic Disease
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S-4048 is a Glucose-6-phosphatase (G6Pase) inhibitor with an IC50 value of 9.4 nM for rat microsomes.
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-
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- HY-78144
-
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IAP
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Inflammation/Immunology
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4-Methylsalicylic acid is a salicylic acid. 4-Methylsalicylic acid derivative is a selective tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibitor .
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-
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- HY-N3267
-
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Phosphatase
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Metabolic Disease
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Methyl pseudolarate B, a natural diterpenoid, is a protein tyrosine phosphatase 1B (PTP1B) (Phosphatase) inhibitor with an IC50 value of 10.9 μM .
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-
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- HY-19776
-
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Phosphatase
|
Cancer
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3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
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-
-
- HY-N12613
-
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Phosphatase
|
Inflammation/Immunology
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Sydowimide A is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), T-cell protein tyrosine phosphatase (TCPTP) and leukocyte common antigen (CD45), with IC50 values of 1.5, 2.4 and 18.83 μM, respectively .
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-
-
- HY-N4185
-
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Phosphatase
|
Neurological Disease
|
Licoflavone A is a flavonoid isolated from the roots of Glycyrrhiza uralensis, inhibits protein tyrosine phosphatase-1B (PTP1B), with an IC50 of 54.5 μM .
|
-
-
- HY-133511
-
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Phosphatase
|
Cancer
|
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity .
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-
-
- HY-B1194
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(±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829
|
Parasite
Phosphatase
Antibiotic
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Infection
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Tetramisole hydrochloride inhibits alkaline phosphatase and is a highly pure antiparasitic agent.
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-
-
- HY-N10186
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-
-
- HY-18983
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(-)-Calyculin A
|
Phosphatase
|
Cancer
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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 .
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-
-
- HY-19695
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L-p-Bromotetramisole oxalate; 6-Bromolevamisole oxalate
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Phosphatase
|
Cancer
|
(-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor.
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-
-
- HY-133146
-
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Phosphatase
Apoptosis
|
Inflammation/Immunology
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DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
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-
-
- HY-128153
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Phosphatase
Apoptosis
|
Cancer
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Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects .
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-
-
- HY-128978
-
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Phosphatase
|
Metabolic Disease
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(E,E)-RAMB4 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1 .
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-
-
- HY-155374
-
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Phosphatase
Apoptosis
|
Cancer
|
PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer .
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-
-
- HY-W013478
-
|
Phosphatase
|
Cancer
|
PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect .
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-
-
- HY-15832
-
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Phosphatase
|
Cancer
|
GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.
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-
-
- HY-B0579
-
-
-
- HY-112139
-
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Phosphatase
|
Others
|
4-(Bromoacetyl)phenoxyacetic acid (PTP inhibitor III) is a protein tyrosine phosphatase (PTP) inhibitor .
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-
-
- HY-135564B
-
|
Phosphatase
|
Cancer
|
(Rac)-RK-682, a racemate of RK-682, is a protein tyrosine phosphatases (PTPases) inhibitor. (Rac)-RK-682 inhibits protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B) with IC50s of 8.6 μM, 12.4 μM, and 0.7 μM, respectively .
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-
-
- HY-123846
-
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Phosphatase
|
Cardiovascular Disease
|
MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs) .
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-
-
- HY-19820A
-
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Akt
Ser/Thr Protease
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Neurological Disease
Cancer
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NSC45586 sodium is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 sodium targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 sodium can activate AKT in neurons .
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-
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- HY-19820
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Akt
Ser/Thr Protease
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Neurological Disease
Cancer
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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 .
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-
-
- HY-12312
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-
-
- HY-W008385
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-
-
- HY-18685
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-
-
- HY-15842
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-
-
- HY-125259
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-
-
- HY-162355
-
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SHP2
|
Cancer
|
SHP2-IN-27 (compound 28) is an allosteric inhibitor of tyrosine phosphatase SH2 .
|
-
-
- HY-111489B
-
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Phosphatase
|
Metabolic Disease
|
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
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-
-
- HY-111489A
-
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Phosphatase
|
Metabolic Disease
|
LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
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-
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- HY-111489
-
|
Phosphatase
|
Metabolic Disease
|
LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
-
- HY-101510
-
|
Phosphatase
|
Cancer
|
F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.
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-
-
- HY-113821
-
|
Phosphatase
|
Others
|
1-Naphthyl phosphate potassium salt is a non-specific phosphatase inhibitor. 1-Naphthyl phosphate potassium salt decreases the splice-correcting effect .
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-
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- HY-163408
-
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Phosphatase
|
Others
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ALP-IN-1 (Compound 7e) is an alkaline phosphatase (ALP) inhibitor (IC50 = 0.308 µM) .
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-
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- HY-100463
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-
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- HY-19779
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|
|
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JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
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-
-
- HY-13588
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SCE-129 sodium
|
Bacterial
Antibiotic
|
Infection
|
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
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- HY-13588B
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SCE-129 sodium hydrate
|
Antibiotic
Bacterial
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Infection
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Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
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-
-
- HY-115496
-
-
-
- HY-10704
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PTP1B inhibitor
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
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-
-
- HY-18756
-
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SHP2
Phosphatase
Apoptosis
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Others
|
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively . NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26) .
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-
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- HY-18756A
-
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SHP2
Phosphatase
Apoptosis
|
Cancer
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NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively . NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26) .
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- HY-W014622
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DNA/RNA Synthesis
|
Cancer
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CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
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-
-
- HY-N8789
-
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Phosphatase
|
Others
|
2-Hydroxymethyl-3-hydroxyanthraquinone is an antiosteoporotic compound that inhibits osteoclastic tartrate-resistant acid phosphatase (TRAP) activity .
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-
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- HY-W328402
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Others
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Cancer
|
(Rac)-LB-100 is the racemate of LB-100. LB-100 is a protein phosphatase 2A (PP2A) inhibitor .
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- HY-127178
-
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Phosphatase
|
Cancer
|
ML120 analog 1 (compound 1) is a competitive inhibitor with a Ki of 0.69 μM for Hematopoietic protein tyrosine phosphatase (HePTP) .
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- HY-108543
-
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Phosphatase
Apoptosis
|
Cancer
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
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- HY-B0537
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MP-601205
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
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-
- HY-B0537A
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MP-601205 dihydrochloride
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
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-
- HY-139852
-
|
Phosphatase
|
Cancer
|
PLAP-IN-1 is a potent (IC50 = 32 nM) and selective PLAP inhibitor, with no detectable inhibition of tissue non-specific alkaline phosphatase (TNAP) activity.
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- HY-109041
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AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
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- HY-N10649
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
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-
- HY-100462
-
-
- HY-B2203
-
|
Phosphatase
|
Metabolic Disease
|
Calcium glycerophosphate is an inhibitor of intestinal alkaline phosphatase F3. Calcium glycerophosphate is a source of calcium and phosphorus in total parenteral nutrition solutions .
|
-
- HY-B0537C
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MP-601205 dimesylate
|
Antibiotic
Parasite
Fungal
Phosphatase
Bacterial
|
Infection
Cancer
|
Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
|
-
- HY-N10648
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
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-
- HY-P0217
-
-
- HY-100625
-
-
- HY-B0537B
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MP-601205 isethionate
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
|
-
- HY-108599
-
DCP-LA
2 Publications Verification
FR236924
|
PKC
CaMK
Phosphatase
Apoptosis
|
Neurological Disease
|
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 .
|
-
- HY-112478
-
|
Phosphatase
SHP2
|
Cancer
|
PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an 50 of 5.21 μM . PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with 50s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively .
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-
- HY-18667
-
|
Phosphatase
|
Inflammation/Immunology
|
LTV-1 is a potent lymphoid tyrosine phosphatase (LYP) inhibitor in T cells with an IC50 of 508 nM. LTV-1 has the potential for autoimmunity treatment .
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- HY-149943
-
|
Others
|
Inflammation/Immunology
|
PAP-IN-2 (Compound 35) is a purple acid phosphatase (PAP) inhibitor (Kis: 186 nM). PAP-IN-2 can be used for development of anti-osteoporotic compounds .
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- HY-B0537AS
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MP-601205-d4(dihydrochloride)
|
Isotope-Labeled Compounds
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
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-
- HY-B0579S2
-
Cyclosporine A acetate-d4; Ciclosporin A acetate-d4; CsA acetate-d4
|
Isotope-Labeled Compounds
Calcineurin
|
Inflammation/Immunology
|
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 . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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-
- HY-15969
-
Sal003
2 Publications Verification
|
Phosphatase
Apoptosis
|
Cancer
|
Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal .
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- HY-B2006
-
|
|
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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 .
|
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- HY-152168
-
|
PERK
Phosphatase
|
Cancer
|
NSC 295642 is a phosphatase inhibitor. NSC 295642 can significantly increase phospho-Erk cytonuclear differences in intact cells. NSC 295642 can be used for the research of cancer .
|
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- HY-N4317
-
|
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 .
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- HY-100595
-
Stibogluconate trisodium nonahydrate
|
Phosphatase
Parasite
SHP2
|
Cancer
|
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
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-
- HY-112776
-
|
Phosphatase
|
Cancer
|
BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase .
|
-
- HY-112776A
-
|
Phosphatase
|
Cancer
|
BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase .
|
-
- HY-124756
-
SBI-425
1 Publications Verification
|
Phosphatase
|
Cardiovascular Disease
|
SBI-425 is an orally active and potent TNAP (tissue-nonspecific alkaline phosphatase) inhibitor (IC50=16 nM). SBI-425 inhibits TNAP in the vasculature, improving cardiovascular parameters and survival .
|
-
- HY-141523
-
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
Vociprotafib (RMC-4630) is a SHP2 inhibitor, a phosphatase whose inhibition blocks activation of the RAS-RAF-MEK-ERK signaling pathway. Vociprotafib has antitumor activity .
|
-
- HY-123856
-
|
Phosphatase
|
Neurological Disease
|
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward .
|
-
- HY-126730
-
|
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-13756A
-
FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate
|
Phosphatase
FKBP
Autophagy
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
|
-
- HY-N6650
-
|
Phosphatase
|
Metabolic Disease
|
Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.
|
-
- HY-121087
-
BCI-215
2 Publications Verification
|
Phosphatase
|
Cancer
|
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
|
-
- HY-125260
-
|
SHP2
|
Cancer
|
SHP844 is a SHP2 inhibitor with the IC50 of 18.9 µM. SHP2 is a protein tyrosine phosphatase (PTP) that regulates tyrosine phosphorylation levels and is involved in cell proliferation, differentiation and survival .
|
-
- HY-155037
-
|
Others
|
Cancer
|
VE-PTP-IN-1 (compound 2) is a weakly acidic and selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP).VE-PTP-IN-1 is assocaited with vascular homeostasis and angiogenesis.
|
-
- HY-156659
-
|
Phosphatase
|
Others
|
NC1 is a noncompetitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 inhibits LYP by restricting the movement of the WPD-loop. NC1 inhibits LYP-mediated TCR signaling in T cells .
|
-
- HY-101180
-
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-13756
-
-
- HY-N0374
-
|
Glucosidase
|
Metabolic Disease
|
Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
|
-
- HY-P0219
-
|
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-101485
-
Autophagy enhancer-99 hydrobromide
|
Others
|
Neurological Disease
|
AUTEN-99 (hydrobromide) is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14). AUTEN-99 (hydrobromide) crosses the blood-brain barrier and exerts potent neuroprotective effects .
|
-
- HY-18597
-
|
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-W174279
-
|
EGFR
Ras
Phosphatase
|
Metabolic Disease
|
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM) .
|
-
- HY-B0579S
-
Cyclosporine A-d4; Ciclosporin A-d4; CsA-d4
|
Antibiotic
Complement System
Phosphatase
|
Inflammation/Immunology
Cancer
|
Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
|
-
- HY-112800
-
|
Phosphatase
|
Metabolic Disease
|
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity .
|
-
- HY-W008385S
-
-
- HY-15880
-
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy .
|
-
- HY-P1247
-
|
Phosphatase
|
Neurological Disease
|
Calcineurin autoinhibitory peptide is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide could protect neurons from excitatory neuronal death .
|
-
- HY-100786
-
|
|
|
DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect .
|
-
- HY-162119
-
|
Phosphatase
|
Cancer
|
PRL-IN-1 (compound 43) is a phosphatase of regenerating liver (PRL) inhibitor that directly binds the PRL1 trimer interface and obstructs PRL1 trimerization. PRL-IN-1 shows potent anticancer activities .
|
-
- HY-106702
-
CI-920
|
Antibiotic
Phosphatase
|
Cancer
|
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) .
|
-
- HY-12219
-
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-12219A
-
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-109011
-
AQX-1125
|
Phosphatase
|
Cancer
|
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro .
|
-
- HY-115502A
-
(E)-BCI hydrochloride
|
Phosphatase
|
Inflammation/Immunology
|
BCI ((E)-BCI) hydrochloride is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI hydrochloride shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI hydrochloride can be used in inflammatory disease research .
|
-
- HY-115502
-
(E)-BCI
|
Phosphatase
|
Inflammation/Immunology
|
BCI ((E)-BCI) is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI can be used in inflammatory disease research .
|
-
- HY-N1549
-
Naringenin 7-0-glucoside
|
|
|
Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 µM .
|
-
- HY-N4143
-
|
Phosphatase
|
Metabolic Disease
|
Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes .
|
-
- HY-113976A
-
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-18956
-
(E/Z)-Sephin1; (E/Z)-IFB-088
|
|
|
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research .
|
-
- HY-109011A
-
AQX-1125 acetate
|
Phosphatase
|
Cancer
|
Rosiptor (AQX-1125) acetate is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor acetate (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro .
|
-
- HY-108544
-
-
- HY-B0579S3
-
Cyclosporine A-13C2,d4; Ciclosporin A-13C2,d4; CsA-13C2,d4
|
Isotope-Labeled Compounds
Calcineurin
|
Inflammation/Immunology
|
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 . Cyclosporin A also inhibits CD11a/CD18 adhesion .
|
-
- 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-B2006S
-
|
Phosphatase
Bacterial
|
Infection
|
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[1].
|
-
- HY-N2451
-
|
Phosphatase
|
Metabolic Disease
Endocrinology
|
Aloe-emodin-8-O-β-D-glucopyranoside, a compound isolated from Saussrurea lappa, is a moderate inhibitor of human protein tyrosine phosphatase 1B (hPTP1B) with an IC50 of 26.6 μM .
|
-
- HY-P1247A
-
|
Phosphatase
|
Neurological Disease
|
Calcineurin autoinhibitory peptide TFA is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide TFA could protect neurons from excitatory neuronal death .
|
-
- HY-W661499
-
|
Phosphatase
|
Cancer
|
Orellanine is a fungal nephrotoxin. Orellanine is also a competitive inhibitor of alkaline phosphatase. Orellanine induces cell death in proximal tubular cells and in ccRCC cells. Orellanine can be used for research of clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-137135A
-
|
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-149942
-
|
Others
|
Others
|
PAP-IN-1 (compound 28) is an inhibitor of purple acid phosphatases (PAPs), a ubiquitous binuclear metallohydrolase. PAP-IN-1 inhibits mammalian PAP with Ki value of 168 nM. PAP-IN-1 targets to pig PAP with Kic value of 0.17 μM. PAP inhibitors can be used for research of anti-osteoporotic drugs .
|
-
- HY-126326
-
|
Epoxide Hydrolase
|
Metabolic Disease
|
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH .
|
-
- HY-124663
-
|
Protease Activated Receptor (PAR)
|
Cancer
|
CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5b MV, TRAP 5b OX and TRAP 5a OX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively .
|
-
- HY-N10223
-
|
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-106064A
-
U 60257B
|
Leukotriene Receptor
|
Inflammation/Immunology
|
Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells .
|
-
- HY-151591
-
|
Phosphatase
|
Metabolic Disease
|
SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
|
-
- HY-N1230
-
Allolicoisoflavone B
|
|
|
Sophoraisoflavone A (Allolicoisoflavone B) is a nature product that could be isolated from Glycyrrhiza inflate. Sophoraisoflavone A is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 value of 0.80 μM. Sophoraisoflavone A can be used in research of inflammation .
|
-
- HY-121515
-
|
Phosphatase
|
Metabolic Disease
|
DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property .
|
-
- HY-126390
-
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-121515A
-
|
Phosphatase
|
Metabolic Disease
|
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property .
|
-
- HY-15756
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes .
|
-
- HY-N8200
-
-
- HY-108196
-
|
Phosphatase
|
Endocrinology
|
PTP1B-IN-15 is a potent and selective inhibitor of protein tyrosine phosphatase 1B (PTP1B). PTP1B-IN-15 has the potential for the research of type II diabetes and obesity .
|
-
- HY-101964
-
|
SHP2
Phosphatase
|
Cancer
|
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively .
|
-
- HY-111022
-
Sephin1; IFB-088
|
Phosphatase
|
Infection
Inflammation/Immunology
|
Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
|
-
- HY-130631
-
|
SHP2
|
Cancer
|
SHP2-IN-5 (compound 1) is an inhibitor of SHP2 (IC50: 97 nM). SHP2 is a non-receptor protein tyrosine phosphatase associated with cell growth and proliferation. SHP2-IN-5 has the potential to inhibit cancer and SHP2-related human diseases .
|
-
- HY-N7599
-
|
Phosphatase
Glucosidase
|
Metabolic Disease
|
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research .
|
-
- HY-145741
-
|
Antibiotic
|
Infection
|
MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacterium tuberculosis survival and infection burden .
|
-
- HY-N10378
-
|
Phosphatase
|
Neurological Disease
Metabolic Disease
|
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression .
|
-
- HY-N12177
-
|
Phosphatase
|
Metabolic Disease
|
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively .
|
-
- HY-110365
-
Sephin1 Carbonate; IFB-088 Carbonate
|
Phosphatase
|
Infection
|
Icerguastat (Sephin1) Carbonate, a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat Carbonate inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
|
-
- HY-13756S
-
FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2
|
Phosphatase
FKBP
Bacterial
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
|
-
- HY-126246
-
|
Phosphatase
|
Cancer
|
CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase .
|
-
- HY-N2511
-
|
Cholinesterase (ChE)
Phosphatase
Endogenous Metabolite
|
Metabolic Disease
|
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively .
|
-
- HY-133512
-
|
Phosphatase
|
Cancer
|
NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells .
|
-
- HY-141800
-
|
Others
|
Others
|
MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC50 values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively . (A family of human MAPK-specific protein tyrosine phosphatases)
|
-
- HY-144717
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-18 is an orally active complete mixed type protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 35.2 μM. PTP1B-IN-18 can be used for type 2 diabetes research .
|
-
- HY-144718
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-17 (Compound 45), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 30.2 μM. PTP1B-IN-17 can be used for the research of type 2 diabetes.
|
-
- HY-144716
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-19 (Compound 43), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 23.3 μM. PTP1B-IN-19 can be used for the research of type 2 diabetes.
|
-
- HY-144713
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-16 (Compound 46), a potential selective benzimidazole derivative, acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 12.6 μM. PTP1B-IN-16 can be used for the research of type 2 diabetes.
|
-
- HY-W181102
-
|
Calcineurin
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17) .
|
-
- HY-118567
-
BMOV
|
SHP2
Phosphatase
|
Metabolic Disease
|
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer .
|
-
- HY-15486
-
|
Phosphatase
HSV
Autophagy
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation . Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis . Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5 .
|
-
- HY-N6663
-
|
COX
|
Inflammation/Immunology
|
3-Carene is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene inhibits nociceptive stimulus-induced inflammatory infiltrates and COX-2 overexpression, and with antinociceptive effect. 3-Carene stimulates the activity and expression of alkaline phosphatase that is an early phase marker of osteoblastic differentiation .
|
-
- HY-153018
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-22, a ZINC02765569 derivative, is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor. PTP1B-IN-22 has PTP1B inhibition and glucose uptake in skeletal muscle L6 myotubes .
|
-
- HY-N3734
-
|
Beta-secretase
Phosphatase
|
Neurological Disease
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
|
-
- HY-149865
-
|
Phosphatase
Fluorescent Dye
|
Cancer
|
TPE-1p is a cascade-activated AIEgen-peptide probe. TPE-1p self-assembles in aqueous solution to exhibit bright fluorescence in response to alkaline phosphatase (ALP) and ChT-L. TPE-1p can be utilized to noninvasively assess the inhibition efficiency of a ChT-L inhibitor in cells .
|
-
- HY-147071
-
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-123966
-
|
Phosphatase
|
|
MY33-3 is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction .
|
-
- HY-123966A
-
|
Phosphatase
|
Neurological Disease
|
MY33-3 hydrochloride is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 hydrochloride also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 hydrochloride can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction .
|
-
- HY-137092
-
|
SHP2
Phosphatase
|
Cancer
|
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .
|
-
- HY-120159
-
|
SHP2
Phosphatase
|
Cancer
|
GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity .
|
-
- HY-100683
-
|
Phosphatase
|
Cancer
|
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells .
|
-
- HY-157139
-
|
Carbonic Anhydrase
Phosphatase
|
Inflammation/Immunology
|
ALP/Carbonic anhydrase-IN-1 (Compound 1e) is a dual carbonic anhydrase (CA) and alkaline phosphatase (ALP) inhibitor. ALP/Carbonic anhydrase-IN-1 shows IC50 values of 0.44 µM, 1.61 µM, 0.51 µM, and 0.107 µM for CA-II, CA-IX, CA-XII, and ALP, respectively .
|
-
- HY-126304
-
|
Phosphatase
Endogenous Metabolite
ERK
|
Metabolic Disease
|
β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells .
|
-
- HY-P3355
-
|
iGluR
|
Neurological Disease
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-N2511S
-
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
Phosphatase
Endogenous Metabolite
|
|
Trimyristin--d15 is the deuterium labeled Trimyristin. Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
|
-
- HY-113612A
-
|
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-124591
-
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling .
|
-
- HY-D0886
-
|
Phosphatase
Endogenous Metabolite
ERK
|
Metabolic Disease
Cancer
|
β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells .
|
-
- HY-124896
-
6-Geranylnaringenin; Mimulone
|
Phosphatase
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
- HY-155558
-
|
Antibiotic
|
Infection
|
MptpB-IN-2 (compound 20) is a selective mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitor with IC50s of 0.64 μM, 4.06 μM and 4.14 μM for MptpB, MptpA and PTP1B, respectively. MptpB-IN-2 shows weak antituberculosis activity with a MIC of 64.9 μM for Mtb H37Rv .
|
-
- HY-123931
-
ZLDI-8
1 Publications Verification
|
Notch
Phosphatase
Apoptosis
|
Cancer
|
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM .
|
-
- HY-155848
-
|
Phosphatase
|
Cancer
|
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
|
-
- HY-139598
-
|
Phospholipase
|
Cardiovascular Disease
|
LFHP-1c is an PGAM5 inhibitor with neuroprotective activity in brain ischemic stroke. LFHP-1c protects blood-brain barrier integrity from ischemia-induced injury. LFHP-1c binds to endothelial PGAM5 to inhibit the activity of PGAM5 phosphatase and the interaction of PGAM5 with NRF2. LFHP-1c exhibits in vitro and in vivo protection .
|
-
- HY-155847
-
|
Phosphatase
|
Cancer
|
LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress. LYP-IN-3 activates T-cell and inhibits M2 macrophage polarization, but upregulates PD-1/PD-L1 expression. LYP-IN-3 can be leveraged with PD-1/PD-L1 inhibitor, for futher cancer immunotherapy .
|
-
- HY-120327
-
KY-226
1 Publications Verification
|
Phosphatase
|
Neurological Disease
Metabolic Disease
|
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
|
-
- HY-139693
-
|
Phosphatase
|
Inflammation/Immunology
Cancer
|
PTPN22-IN-1 is a potent PTPN22 inhibitor (IC50=1.4 µM; Ki=0.50 µM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses . From WO2021007491A1 compound L-1.
|
-
- HY-P3354
-
|
iGluR
|
Neurological Disease
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-N6785
-
|
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
-
|
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-B0879
-
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-100034
-
DA-3003-1
|
Phosphatase
Histone Methyltransferase
|
Cancer
|
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
|
-
- HY-128769
-
|
CDK
|
Cancer
|
M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09 μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of 0.53 μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research .
|
-
- HY-118529
-
|
Phosphatase
|
Cancer
|
JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1 .
|
-
- HY-115760
-
|
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-B0879A
-
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-18686
-
|
|
|
AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 µM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes .
|
-
- HY-103693
-
NAZ2329
1 Publications Verification
|
Phosphatase
|
Cancer
|
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
|
-
- HY-103241
-
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response . Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
|
-
- HY-101115
-
|
PI3K
|
Cancer
|
PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors .
|
-
- HY-153335
-
|
Phosphodiesterase (PDE)
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Enpp-1-IN-16 (compound 54) is an ENPP1 inhibitor. Enpp-1-IN-16 has the potential to study cancer, especially in cases of high ENPP1 expression or elevated cytoplasmic DNA levels. Enpp-1-IN-16 can also be used in other diseases mediated by ENPP1, such as bacterial or viral infections, insulin resistance and type II diabetes, chondrocalcinosis and osteoarthritis, calcium pyrophosphate deposition disorder (CPPD), low Phosphatase disease and soft tissue calcification disorders .
|
-
- HY-136065
-
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity .
|
-
- HY-152247
-
|
MAP3K
|
Cancer
|
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .
|
-
- HY-122818
-
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity .
|
-
- HY-123960A
-
|
Phosphatase
|
Neurological Disease
|
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 .
|
-
- HY-123960
-
|
Phosphatase
|
Neurological Disease
|
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 .
|
-
- 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
-
|
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-149254
-
|
Phosphatase
Aldose Reductase
|
Metabolic Disease
|
PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels .
|
-
-
-
HY-L081
-
|
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 |
Type |
-
- HY-D0852
-
|
Biochemical Assay Reagents
|
Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
|
-
- HY-19695
-
L-p-Bromotetramisole oxalate; 6-Bromolevamisole oxalate
|
Biochemical Assay Reagents
|
(-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0217
-
-
- HY-P1247
-
|
Phosphatase
|
Neurological Disease
|
Calcineurin autoinhibitory peptide is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide could protect neurons from excitatory neuronal death .
|
-
- HY-P2040
-
|
Peptides
|
Cancer
|
Nodularin is a potent hepatotoxin, tumor promoter, and protein phosphatase inhibitor .
|
-
- HY-P0219
-
|
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-P1247A
-
|
Phosphatase
|
Neurological Disease
|
Calcineurin autoinhibitory peptide TFA is a selective inhibitor of Ca 2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide TFA could protect neurons from excitatory neuronal death .
|
-
- HY-P3355
-
|
iGluR
|
Neurological Disease
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-P3354
-
|
iGluR
|
Neurological Disease
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-K0022
-
|
Phosphatase Inhibitor Cocktail II effectively inhibits acid and alkaline phosphatases as well as protein tyrosine phosphatases(PTPs).
|
-
- HY-K0021
-
Maximum Cited Publications
351 Publications Verification
|
Phosphatase Inhibitor Cocktail I effectively inhibits alkaline phosphatases and serine/threonine protein phosphatases such as PP1 and PP2A.
|
-
- HY-K0023
-
|
Phosphatase Inhibitor Cocktail III effectively inhibits serine/threonine and alkaline phosphatases.
|
-
- HY-K0013
-
|
MCE Protease and Phosphatase Inhibitor Cocktail (EDTA-Free, 10× in ddH2O) protects protein from degradation by endogenous proteases released during protein extraction and purification.
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N4185
-
-
-
- HY-N3267
-
-
-
- HY-N12613
-
-
-
- HY-N10186
-
-
-
- HY-P2040
-
-
-
- HY-B0579
-
-
-
- HY-W008385
-
-
-
- HY-N8789
-
-
-
- HY-N10649
-
-
-
- HY-N10648
-
-
-
- HY-N4317
-
-
-
- HY-13756A
-
-
-
- HY-N6650
-
-
-
- HY-13756
-
-
-
- HY-N0374
-
-
-
- HY-P0219
-
-
-
- HY-106702
-
-
-
- HY-N4143
-
-
-
- HY-N2451
-
-
-
- HY-W661499
-
-
-
- HY-N10223
-
-
-
- HY-N8200
-
-
-
- HY-N7599
-
-
-
- HY-N10378
-
-
-
- HY-N12177
-
-
-
- HY-N2511
-
-
-
- HY-N6663
-
-
-
- HY-N3734
-
-
-
- HY-126304
-
-
-
- HY-D0886
-
-
-
- HY-124896
-
6-Geranylnaringenin; Mimulone
|
Paulownia tomentosa (Thunb.) Steud.
Scrophulariaceae
Plants
|
Phosphatase
Apoptosis
Autophagy
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
-
- HY-N6785
-
|
Structural Classification
Animals
Ketones, Aldehydes, Acids
Marine natural products
Source classification
Other marine organisms
|
Phosphatase
Apoptosis
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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 .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0537AS
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Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
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- HY-B0579S
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Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
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- HY-B0579S2
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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 . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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- HY-W008385S
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H-HoArg-OH-d4 is a deuterium labeled H-HoArg-OH (HY-W008385). H-HoArg-OH, a homologue arginine, is a strong inhibitor of human bone and liver alkaline phosphatase.
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- HY-B0579S3
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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 . Cyclosporin A also inhibits CD11a/CD18 adhesion .
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- HY-B2006S
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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[1].
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- HY-13756S
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Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
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- HY-N2511S
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Trimyristin--d15 is the deuterium labeled Trimyristin. Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
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Cat. No. |
Product Name |
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Classification |
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- HY-135699
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TD52
1 Publications Verification
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Alkynes
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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.
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- HY-135699A
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Alkynes
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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.
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