Blog of Signaling Pathways

Bafetinib is a second generation tyrosine kinase inhibitor

3826 views | Jan 06 2014

Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells [Read the Full Post]

AZD1080 is a selective orally active brain permeable GSK3 inhibitor

0 views | Jan 06 2014

AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. [Read the Full Post]

Tariquidar is a P glycoprotein inhibitor undergoing research

4407 views | Dec 30 2013

Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. [Read the Full Post]

Zosuquidar is a compound of antineoplastic drug

4081 views | Dec 30 2013

Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. [Read the Full Post]

PP242 is a new small molecule protein kinase inhibitor

0 views | Dec 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]

Maraviroc is an antiretroviral drug in the CCR5 receptor

3544 views | Dec 29 2013

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

Perifosine is structurally related to miltefosine

3484 views | Dec 26 2013

Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. [Read the Full Post]

NU7441 is a potent novel DNA PK inhibitor

2752 views | Dec 26 2013

NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM. [Read the Full Post]

Dasatinib is a rescription medicine used to treat adults

3434 views | Dec 25 2013

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively. [Read the Full Post]

Docetaxel is a clinically well established anti mitotic chemotherapy medication

2503 views | Dec 25 2013

Docetaxel, an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules. [Read the Full Post]

Neratinib is a highly selective HER2 and EGFR inhibitor

3381 views | Dec 25 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]

EPZ5676 is an Sadenosyl methionine competitive inhibitor

2283 views | Dec 24 2013

EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. [Read the Full Post]

Brefeldin A used to enhance intracellular cytokine staining signals

3143 views | Dec 23 2013

Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. [Read the Full Post]

SB939 is a novel histone deacetylas inhibitor with improved

4259 views | Dec 23 2013

SB939 is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. [Read the Full Post]

Dasatinib is a cancer drug produced by Bristol Myers Squibb

3817 views | Dec 23 2013

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively. [Read the Full Post]

ABT 737 is a small molecule that acts as a selective inhibitor of Bcl 2

2851 views | Dec 23 2013

ABT-737 shows low activity to Bcl-B and no effects to Mcl-1 and BFL-1. [Read the Full Post]

ABT 888 is a potential anti cancer drug acting as a PARP inhibitor

4499 views | Dec 20 2013

ABT-888 is inactive to SIRT2 (>5 μM) .ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [Read the Full Post]

Dapagliflozin is a drug used to treat type 2 diabetes

0 views | Dec 20 2013

Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. [Read the Full Post]

Deforolimus is a small molecule inhibitor of the mammalian target of rapamycin

2364 views | Dec 19 2013

Ridaforolimus is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. [Read the Full Post]

Wnt C59 was first disclosed in patent WO2010101849 as a potent

4065 views | Dec 19 2013

Wnt-C59 is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. [Read the Full Post]