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Blog of Signaling Pathways

FTY720 is phosphorylated by sphingosine kinase type 2

2592 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

3660 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]

Staurosporine is a potent PKC inhibitor with IC50

5127 views | Sep 24 2013

Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. [Read the Full Post]

Sorafenib is used to treat advanced renal cell carcinoma

2351 views | Sep 22 2013

Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. [Read the Full Post]

PHA848125 is a spectrum selective multi kinase inhibitor of cyclin dependent kinases

2274 views | Sep 17 2013

PHA-848125 is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2. [Read the Full Post]

Y27632 is a selective inhibitor of the Rhoassociated kinase p160ROCK

4823 views | Sep 12 2013

Y27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively, as well as PKA activated by another Rho-family GTPase member, Cdc42. [Read the Full Post]

NPS2143 is a novel potent and selective antagonist of Ca

2456 views | Sep 10 2013

n rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels. [Read the Full Post]

PLX4032 is a highly selective inhibitor of BRAF kinase activity

2446 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

2278 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

2256 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

3331 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

2560 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

2341 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

3112 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

1836 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

3428 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

2550 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

2486 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

2666 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

2279 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]