Phosphatase Inhibitor

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.

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.

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.

H-HomoArg-OH (L-Homoarginine) is an orally active endogenous non-protein amino acid. H-HomoArg-OH acts as a weak alternative substrate for NOS and interferes with NO production, selectively inhibits tissue-nonspecific alkaline phosphatase (TNAP), and suppresses the uptake of arginine by y⁺-type transporters (system y⁺). H-HomoArg-OH increases tissue hArg concentrations in vivo, regulates amino acid homeostasis, and improves renal function and pathological features of diabetic nephropathy. H-HomoArg-OH can be used in studies related to diabetes and cardiomyopathy.

Domiphen bromide is a cationic active quaternary ammonium salt and also an inhibitor of HERG channels (IC₅₀: 9 nM), aminopeptidase-like enzymes, Escherichia coli alkaline phosphatase, and α-chymotrypsin. Domiphen bromide has multiple activities such as antibacterial, antimalarial, and disinfectant properties, and it is also a synergist of Colistin (HY-113678). Domiphen bromide can be used as a chemical preservative and a cationic surfactant, and it can also be used in the research of bacterial infectious diseases such as pharyngitis, thrush, and oral ulcers.

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.

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.

Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities.

Rubrofusarin gentiobioside (Rrubrofusarin-6-β-gentiobioside) is an orally active weak inhibitor of PTP1B and MAO-A (IC₅₀ >100 μM), and its glycosylation modification results in lower biological activity than its aglycone Rubrofusarin (HY-130307). Rubrofusarin gentiobioside promotes AMPK phosphorylation in an LKB1-independent manner and inhibits the mTOR signaling pathway, thereby downregulating the expressions of PPARγ, C/EBPα, as well as FAS, LPL and aP2. Rubrofusarin gentiobioside inhibits lipid accumulation, reduces body weight and epididymal white adipose tissue volume, improves fatty liver, and shows no cytotoxicity to hepatocytes. Rubrofusarin gentiobioside is widely used in obesity-related studies.

MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 reduces NF-κB p65 expression. MY10 activates tyrosine phosphorylation of c-Met. MY10 prevents the alcohol-induced downregulation of Ptprz1 and Alk expression. MY10 attenuates binge-like ethanol consumption and ethanol reward. MY10 can be used in the study of neurological and vascular diseases.

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC₅₀ of 15.7 nM and a K_d 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.

PGAM1-IN-1 is a phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC₅₀ of 6.4 μM.

Quercetagitrin (Quercetagetin-7-O-glucoside) is a natural product that can be isolated from the African marigold (Tagetes erecta). Quercetagitrin has anti-inflammatory activity. Quercetagitrin inhibits Tau accumulation. Quercetagitrin can reverse neuroinflammation and cognitive deficits in P301S-Tau transgenic mouse model through inhibiting NF-κB activation. Quercetagitrin is a dual-target inhibitor of PTPN6 (IC₅₀ = 1 μM) and PTPN9 (IC₅₀ = 1.7 μM). Quercetagitrin enhances glucose uptake by mature C2C12 myoblasts. Quercetagitrin can be studied in research for Alzheimer’s disease and type 2 diabetes.

Y29 is a potent PFKFB3 inhibitor with an IC₅₀ of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a K_i value of 0.094 µM. Y29 exhibits antitumor effects against cervical cancer.

CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research.

M5N36 is a potent and selective Cdc25C inhibitor with IC₅₀ values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2.

Tacrolimus-¹³C,d₂ (FK506-¹³C,d₂) is the ¹³C, deuterated-labeled Tacrolimus (HY-13756). Tacrolimus (FK506), a molecular glue, 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.

Tacrolimus (Standard) (FK506 (Standard); Fujimycin (Standard); FR900506 (Standard)) is the analytical standard of Tacrolimus (HY-13756). This product is intended for research and analytical applications. Tacrolimus (FK506), a molecular glue, 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.

ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC₅₀s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.

KF-52 is a phosphofructokinase-1 (PFK1) inhibitor with an IC₅₀ value of 2.1 μM. KF-52 significantly increases the ratio of oxygen consumption rate (OCR) to extracellular acidification rate (ECAR). KF-52 is applicable to research related to mitochondrial dysfunction.