Blog of Signaling Pathways

IOX2 is a potent inhibitor of HIF 1 prolyl hydroxylase 2 with IC50

4119 views | Oct 29 2013

IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. [Read the Full Post]

PP242 is a new small molecule protein kinase inhibitor

2326 views | Oct 29 2013

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. [Read the Full Post]

VX809 is an experimental drug for the treatment of cystic fibrosis

2490 views | Oct 28 2013

VX-809 acts at the level of the ER to allow a fraction of the F508del-CFTR to adopt a properly folded form, to exit the ER and mobilize to the cell surface for normal functioning. [Read the Full Post]

Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma

1908 views | Oct 28 2013

In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. [Read the Full Post]

Trichostatin A is an organic compound that serves as an antifungal antibiotic

3320 views | Oct 25 2013

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM – HDAC8 is the only known member of the HDAC-family that is not affected by TSA. [Read the Full Post]

AM803 is under development as an oral controller for the treatment

2250 views | Oct 25 2013

GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma. [Read the Full Post]

CGK733 was a synthetic chemical substance which was reported in 2006

3760 views | Oct 23 2013

CGK733 is able to confer robust growth to senescent cells that have ceased proliferation. [Read the Full Post]

Tariquidar is a P glycoprotein inhibitor undergoing research as an adjuvant

3470 views | Oct 23 2013

Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM, reverses drug resistance in MDR cell Lines. [Read the Full Post]

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

2470 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

1851 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

2826 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

2459 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

2011 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

2380 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

2961 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

2543 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

3588 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]