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Blog of Signaling Pathways

PLX4032 is a highly selective inhibitor of BRAF kinase activity

2461 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

2309 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

2283 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]

MS275 strongly inhibits HDAC1 and HDAC3 with IC50

3361 views | Aug 29 2013

MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [Read the Full Post]

ARQ197 has been shown to prevent HGF induced cellular responses

2577 views | Aug 26 2013

ARQ-197 is the first non-ATP-competitive c-Met inhibitor withKi of 0.355 μM [Read the Full Post]

LY2886721 is used to treat Alzheimers Disease in preclinical experiments

2356 views | Aug 23 2013

LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease. [Read the Full Post]

Triciribine was initially described as a DNA synthesis inhibitor

3133 views | Aug 21 2013

Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM [Read the Full Post]

RAD001 is specific inhibitors mTOR signal

1861 views | Aug 19 2013

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]

Tideglusib might be useful for slowing atrophy rates

3451 views | Aug 15 2013

Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 1/2. [Read the Full Post]

Roscovitine is an experimental drug candidate

2571 views | Aug 12 2013

Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. [Read the Full Post]

MS275 is a benzamide histone deacetylase inhibitor

2507 views | Aug 08 2013

MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. [Read the Full Post]

Sunitinib was the first cancer drug simultaneously

2695 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

2300 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

2294 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

2449 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

2382 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

2314 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

3055 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

2852 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

2367 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]