Blog of Signaling Pathways

OSI 930 is a novel inhibitor of the receptor tyrosine kinases Kit

2589 views | Oct 22 2013

OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. [Read the Full Post]

PP242 is an inhibitor at the kinase domain of the mammalian target of rapamycin

1936 views | Oct 22 2013

PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. [Read the Full Post]

Semagacestat was compared with placebo in more than 2600 patients

3028 views | Oct 21 2013

Semagacestat reduces the secretion of Aβ42, Aβ40 and Aβ38 from H4 human glioma cells stably overexpressing human wild-type APP into the culture medium [Read the Full Post]

Neratinib is a tyrosine kinase inhibitor under investigation

2661 views | Oct 21 2013

Neratinib weakly inhibits tyrosine kinases KDR and Src with IC50 of 0.8 μM and 1.4 μM, respectively, being 14- and 24-fold less active compared with HER2. [Read the Full Post]

PD0325901 is selective and non ATP competitive MEK inhibitor

2116 views | Oct 17 2013

PF0325901 shows higher permeability than CI-1040, another MEK inhibitor. PD0325901 should be able to achieve higher systemic exposures than CI-1040. [Read the Full Post]

PHA 665752 is a potent selective and ATP competitive c Met inhibitor

2496 views | Oct 17 2013

PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. [Read the Full Post]

SB203580 is a selective inhibitor of p38 mitogen activated protein kinase

3124 views | Oct 16 2013

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. [Read the Full Post]

SANT1 is a potent inhibitor of Sonic hedgehog signaling

0 views | Oct 16 2013

SANT-1 inhibits wild type and oncogenic Smo with equal potency. [Read the Full Post]

U0126 is a highly selective inhibitor of both MEK1 and MEK2

0 views | Oct 11 2013

U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. [Read the Full Post]

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

0 views | Oct 09 2013

ABT-888 is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. It is inactive to SIRT2. [Read the Full Post]

FTY720 is phosphorylated by sphingosine kinase type 2

2683 views | Sep 30 2013

The inhibitory effect of S1P is revered by various concentrations of FTY720, with IC50 effect of 173 nM. [Read the Full Post]

Nutlin3 inhibits the MDM2 p53 interaction and activates p5

3776 views | Sep 26 2013

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. [Read the Full Post]

Staurosporine is a potent PKC inhibitor with IC50

5355 views | Sep 24 2013

Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. [Read the Full Post]

Sorafenib is used to treat advanced renal cell carcinoma

2428 views | Sep 22 2013

Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. [Read the Full Post]

PHA848125 is a spectrum selective multi kinase inhibitor of cyclin dependent kinases

2353 views | Sep 17 2013

PHA-848125 is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2. [Read the Full Post]

Y27632 is a selective inhibitor of the Rhoassociated kinase p160ROCK

4972 views | Sep 12 2013

Y27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. [Read the Full Post]

NPS2143 is a novel potent and selective antagonist of Ca

2577 views | Sep 10 2013

n rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels. [Read the Full Post]

PLX4032 is a highly selective inhibitor of BRAF kinase activity

2548 views | Sep 05 2013

PLX4032 is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM. [Read the Full Post]

SANT1 is a potent inhibitor of Sonic hedgehog signaling

2389 views | Sep 02 2013

SANT-1 inhibits wild type and oncogenic Smo with equal potency. SANT-1 counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. [Read the Full Post]

STA9090 is a novel synthetic small molecule inhibitor of heat shock protein 90

2337 views | Aug 31 2013

Ganetespib is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. [Read the Full Post]