Blog of Signaling Pathways

Masitinib is a tyrosine kinase inhibitor used in the treatment of mast cell tumors in animals

2773 views | Jul 03 2013

Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. [Read the Full Post]

RAD001 treatment will shrink or slow the growth of the vestibular

1940 views | Jul 01 2013

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. [Read the Full Post]

Tivantinib- is an oral triphosphate competitive cMET inhibitor

2705 views | Jun 28 2013

ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549. [Read the Full Post]

XL-184 is a new chemical entity that inhibits VEGFR2

2657 views | Jun 26 2013

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [Read the Full Post]

TW37 is a Bcl2 inhibitor that has been shown to inhibit the angiogenic potential of endothelial cells

2479 views | Jun 24 2013

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. [Read the Full Post]

MG132 is a specific potent reversible and cell permeable proteasome inhibitor

2776 views | Jun 20 2013

MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. [Read the Full Post]

Veliparib is a potential anti cancer drug acting as a PARP inhibitor

3384 views | Jun 17 2013

ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. [Read the Full Post]

GDC 0941 is a potent inhibitor the PI3 kinase family

2493 views | Jun 13 2013

GDC-0941 is equipotent against PI3Kα and PI3K as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold) [Read the Full Post]

SCH 900776 is targeting cell cycle checkpoint kinase

3011 views | Jun 08 2013

SCH 900776 is not a potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. SCH 900776 shows no significant inhibition of cytochrome P450 human liver microsomal isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. [Read the Full Post]

y27632 is a biochemical tool used in the study of the rho associated protein kinase signaling pathways

5441 views | Jun 07 2013

Oral administration of Y-27632 2HCl at 30 mg/kg significantly decreases the blood pressure in a dose-dependent manner in spontaneous hypertensive rats, renal hypertensive rats, as well as deoxycorticosterone acetate (DOCA)-salt hypertensive rats. [Read the Full Post]

Tideglusib may be useful for slowing atrophy rates

3901 views | Jun 05 2013

Tideglusib (50 mg/kg) injected into the adult male Wistar rats hippocampus dramatically reduces kainic acid-induced inflammation and has a neuroprotective effect in the damaged areas of the hippocampus. [Read the Full Post]

FTY720 is an immunomodulating drug, approved for treating multiple sclerosis

2927 views | Jun 03 2013

Fingolimod is a sphingosine 1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction. [Read the Full Post]

Ouabain isolated from plants is widely used by scientists in in vitro studies

2930 views | May 30 2013

In many non rodent species, low concentrations of this substance (i.e., in the subnanomolar range) may stimulate the Na-K-ATPase. The mechanism of the stimulatory effect is not understood and remains controversial. Further, the issue in rodents is more complicated because there are different isoforms of the Na-K-ATPase - some of which are very sensitive to ouabain while others are not. [Read the Full Post]

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM

2537 views | May 28 2013

INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. [Read the Full Post]

Learn about the prescription medication Methazolamide

2508 views | May 26 2013

Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. [Read the Full Post]

Effects of oral administration of methazolamide on intraocular pressure

2436 views | May 22 2013

In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics [Read the Full Post]

Rucaparib is a PARP inhibitor being investigated as a potential anticancer agent

3188 views | May 20 2013

Rucaparib also reduces the migration of some cancer and normal cells in culture.It can be taken orally in tablet form. [Read the Full Post]

Motesanib is an experimental drug candidate

2815 views | May 16 2013

Motesanib Diphosphate has broad activity against the human VEGFR family, and displays >1000 selectivity against EGFR, Src, and p38 kinase. [Read the Full Post]

Ouabain is found in the ripe seeds of African plants

3101 views | May 14 2013

It is well understood that the classical mechanism of action of ouabain involves its binding to and inhibition of the plasma membrane Na+/K+-ATPase (sodium pump) especially at the higher concentrations attainable in vitro or with intravenous dosage. [Read the Full Post]

MK 801 has a great deal of potential to be used in research in creating animal models of schizophrenia

3430 views | May 10 2013

MK-801 has a great deal of potential to be used in research in creating animal models of schizophrenia. Unlike dopaminergic agonists, which mimic only the positive symptoms of schizophrenia, a single injection of MK801 was successful in modelling both the positive and negative symptoms of schizophrenia. [Read the Full Post]