Blog of Signaling Pathways

Sunitinib was the first cancer drug simultaneously

2668 views | Aug 06 2013

Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. [Read the Full Post]

U0126 is a highly selective inhibitor of both MEK1 and MEK2

2282 views | Aug 02 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]

AMG517 is a potent and selective transient receptor potential TRPV1 antagonist

2284 views | Jul 31 2013

Oral administration of AMG 517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. [Read the Full Post]

MRS2578 is a selective antagonist of P2Y6 nucleotide receptors

2436 views | Jul 29 2013

MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. [Read the Full Post]

Trametinib had good results for V600E mutated metastatic melanoma

2363 views | Jul 25 2013

GSK1120212 inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, with IC50 ranging from 0.92 nM to 3.4 nM. GSK1120212 demonstrates no inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. [Read the Full Post]

PHA767491 is a newly discovered type of antitumor drugs

2306 views | Jul 23 2013

PHA-767491 displays approximately 20-fold selectivity for Cdk1, Cdk2 and GSK3-β, 50-fold selectivity for MK2 and Cdk5 and 100-fold selectivity for PLK1 and CHK2. [Read the Full Post]

Vicriviroci s a pyrimidine CCR5 entry inhibitor of HIV1

3013 views | Jul 20 2013

Vicriviroc binds with higher affinity to CCR5 versus SCH-C (SCH-351125) in competition binding assays with Ki value of 0.8 nM versus 2.6 nM. [Read the Full Post]

PD168393 is a strongly effective EGFR inhibitors

2829 views | Jul 18 2013

PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. [Read the Full Post]

TOK001 is an experimental drug being developed by Tokai Pharmaceuticals

2350 views | Jul 16 2013

Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. [Read the Full Post]

TWS119 is thought to bind GSK with high affinity

3889 views | Jul 11 2013

Treatment of a monolayer of P19 cells with 1 μM TWS119 causes 30–40% cells to differentiate specifically into neuronal lineages based on counting of TuJ1 positive cells with correct neuronal morphology (up to 60% neuronal differentiation occurred through the standard EB formation protocol with concomitant TWS119 treatment). [Read the Full Post]

Perifosine is a drug candidate being developed for a variety of cancer indications

3031 views | Jul 09 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]

RG108 is a cell permeable specific DNA methyltransferase inhibitor

2667 views | Jul 05 2013

RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. [Read the Full Post]

Masitinib is a tyrosine kinase inhibitor used in the treatment of mast cell tumors in animals

2677 views | Jul 03 2013

Masitinib is a competitive inhibitor against ATP at concentrations ≤500 nM. Masitinib also potently inhibits recombinant PDGFR and the intracellular kinase Lyn, and to a lesser extent, fibroblast growth factor receptor 3. [Read the Full Post]

RAD001 treatment will shrink or slow the growth of the vestibular

1861 views | Jul 01 2013

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. [Read the Full Post]

Tivantinib- is an oral triphosphate competitive cMET inhibitor

2606 views | Jun 28 2013

ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549. [Read the Full Post]

XL-184 is a new chemical entity that inhibits VEGFR2

2544 views | Jun 26 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]

TW37 is a Bcl2 inhibitor that has been shown to inhibit the angiogenic potential of endothelial cells

2413 views | Jun 24 2013

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. [Read the Full Post]

MG132 is a specific potent reversible and cell permeable proteasome inhibitor

2640 views | Jun 20 2013

MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. [Read the Full Post]

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

3272 views | 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]

GDC 0941 is a potent inhibitor the PI3 kinase family

2399 views | 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]