dephosphorylation

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.

Adenosine 5'-diphosphate (ADP) is a naturally occurring nucleotide derived from the dephosphorylation of ATP. Adenosine 5'-diphosphate is essential for cellular metabolism and induces platelet aggregation.

L-Ascorbic acid 2-phosphate trisodium (Sodium ascorbyl phosphate) is utilized in biocatalytic dephosphorylation for electric power generation and electrochemical detection assays.

NFAT Inhibitor (VIVIT peptide) is a cell-permeable compound that selectively inhibits the calcineurin-mediated dephosphorylation of NFAT.

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase AKT mTOR pathway and delays sensitive cells in late mitosis.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).

DDO-3733 is a conformational activator of Protein Phosphatase 5 (PP5) that functions independently of TRP, facilitating the dephosphorylation of downstream substrates.

Bacitracin Zinc is an antibiotic that interferes with the dephosphorylation of C55-isoprenyl pyrophosphate, interference for inhibition of cleavage of Tyr from Met-enkephalin(IC50=10 μM).

A-83586C is a depsipeptide antibiotic from Streptomyces karnatakensis with potent against Gram-positive activity in vitro. A-83586C acts as a highly potent inhibitor of beta-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating o

MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2.

N-Stearoylsphingosine (Cer(d18:1 18:0)) is an amide compound widely found in eukaryotic organisms that enhances protein phosphatase 2A (PP2A) activity by interfering with the binding of PP2A to PP2A inhibitor 2, leading to dephosphorylation of Akt.N-Stearoylsphingosine is used in prostate cancer research.

Q134R, a neuroprotective derivative of hydroxyquinoline, effectively inhibits nuclear factor of activated T-cell (NFAT) signaling and possesses the ability to cross the blood-brain barrier. This compound shows promise for research into Alzheimer's disease (AD) and aging-related disorders[1].

The inositol phosphates are a family of mono- to poly-phosphorylated compounds that act as messengers, regulating cellular functions including cell cycling, apoptosis, differentiation, andmotility. D-myo-Inositol-1,5,6-triphosphate is an intermediate compound, produced by the dephosphorylation of various inositol-tetrakisphosphate forms. The triphosphate can be further metabolized to produce inositol-biphosphate mediators. The biological roles of D-myo-inositol-1,5,6-triphosphate remain to be determined.

D-myo-Inositol-4-phosphate (Ins(4)P1) is a member of the inositol phosphate (InsP) molecular family that play critical roles as small, soluble second messengers in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3, is a second messenger produced in cells by phospholipase C (PLC)-mediated hydrolysis of phosphatidylinositol-4,5-diphosphate. Binding of Ins(1,4,5)P3 to its receptor on the endoplasmic reticulum results in opening of the calcium channels and an increase in intracellular calcium. Ins(4)P1 can be formed by dephosphorylation of Ins(1,4)P2 by inositol polyphosphate 1-phosphatase or dephosphorylated to inositol by inositol monophosphatase.

DiIC1(5) is a signal-off fluorescent probe for the detection of mitochondrial membrane potential disruption. It accumulates in mitochondria and its fluorescence intensity decreases when the mitochondrial membrane potential is disrupted. DilC1(5) has been used in combination with a variety of cell damage and cell death markers to classify nine stages of cell death using flow cytometry. It has also been used as a quencher for the detection of serine phosphorylation and tyrosine dephosphorylation post-translational modifications (PTMs) in quenching resonance energy transfer (QRET) and mTR-FRET applications. It displays excitation/emission maxima of 659/666 nm, respectively.

Succinyladenosine is a biochemical marker of adenylosuccinase (ASL) deficiency. It is formed through the dephosphorylation of intracellular adenylosuccinic acid (S-AMP) by cytosolic 5-nucleotidase [1].

Cyclocreatine, a Creatine analogue, exhibits potent bioenergetic protection by elevating ATP levels. It demonstrates the ability to traverse cell membranes, including the blood-brain barrier, wherein it undergoes phosphorylation and dephosphorylation by creatine kinases.

BTO-1 is a compound known as a Polo-like kinase (Plk) inhibitor, commonly employed for its effectiveness in regulating processes involving phosphorylation and dephosphorylation.

LG308 shows antimicrotubule activity which is a novel synthetic compound. LG308 induces apoptosis, cell death, and significantly suppresses tumor growth that has the potential for the prostate cancer research. LG308 induces arrest of mitotic phase and significantly inhibits progression of G2 M which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2 [1].

CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2 cyclin B, preventing entry into the mitotic phase of the cell cycle.

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).