Blog of Signaling Pathways

SB939 is a pan histone deacetylase inhibitor binding

4229 views | Nov 04 2013

SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. [Read the Full Post]

XL184 is a small molecule inhibitor of the tyrosine kinases c Met

2796 views | Nov 01 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]

IPA 3 is a selective cell permeable Pak1 inhibitor

2233 views | Nov 01 2013

IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of IPA-3. [Read the Full Post]

Torin 1 is a potent and selective inhibitor of mTOR

2625 views | Oct 31 2013

Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. [Read the Full Post]

Nilotinib is indicated for the treatment of adult patients

2690 views | Oct 31 2013

Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression. [Read the Full Post]

This study is designed to evaluate the efficacy and safety of tofacitinib

7127 views | Oct 30 2013

Tofacitinib citrate inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. [Read the Full Post]

MK 8776 is a potent and functionally selective targeting cell

2832 views | Oct 30 2013

SCH 900776 is not a potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. [Read the Full Post]

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

4737 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

2681 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

2906 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

2202 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

3964 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

2609 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

4200 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

4036 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

2800 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

2169 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

3398 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

3044 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

2394 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]