Blog of Signaling Pathways

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

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

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GDC 0941 is a potent inhibitor the PI3 kinase family

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

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SCH 900776 is targeting cell cycle checkpoint kinase

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

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

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

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Tideglusib may be useful for slowing atrophy rates

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

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FTY720 is an immunomodulating drug, approved for treating multiple sclerosis

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

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

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

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

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

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Learn about the prescription medication Methazolamide

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

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Effects of oral administration of methazolamide on intraocular pressure

May 22 2013

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

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