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Blog of Signaling Pathways

Endocrine therapy has become the most important systemic treatment

4168 views | Mar 10 2014

Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. [Read the Full Post]

AGI5198 is the first highly potent and selective mutant IDH1 inhibitor

3052 views | Mar 07 2014

AGI-5198, potently inhibits mutant IDH1 (R132H-IDH1 and R132C-IDH1), but not wildtype IDH1 (IC50 > 100 μM) or any of IDH2 isoforms (R140Q, R172K, wildtype) (IC50 > 100 μM) [Read the Full Post]

Afatinib is a drug approved in much of the world

3762 views | Mar 07 2014

BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. [Read the Full Post]

PCI34051 is a potent histone deacetylase 8 inhibitor

3664 views | Mar 06 2014

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. It has greater than 200-fold selectivity over HDAC1 and 6. [Read the Full Post]

AZD1080 is a novel GSK3 inhibitor rescues synaptic plasticity deficits in rodent brain

3369 views | Mar 06 2014

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM [Read the Full Post]

Y27632 is a biochemical tool used in the study of the ROCK

4989 views | Mar 05 2014

Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC. [Read the Full Post]

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

2924 views | Mar 05 2014

Perifosine combining with temozolomide reduces tumor proliferation in vivo. [Read the Full Post]

Wortmannin is a specific covalent inhibitor of PI3K

2006 views | Mar 03 2014

Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K inhibitors, but little selectivity within the PI3K family. [Read the Full Post]

PD0325901 is a potent MEK inhibitor that suppresses phosphorylation of ERK1

2054 views | Mar 03 2014

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. [Read the Full Post]

At101 was developed to put requirements in place for CPA

2195 views | Mar 03 2014

AT-101 inhibits a panel of different lymphoproliferative malignancies with IC50 ranged from 1.2 μM to 7.4 μM. [Read the Full Post]

Linifanib is a structurally novel potent inhibitor of RTK

3187 views | Mar 03 2014

Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. [Read the Full Post]

Lenalidomide is effective in induring complete response

2351 views | Feb 28 2014

Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM. [Read the Full Post]

Deforolimus is a small molecule inhibitor of the mammalian target

1950 views | Feb 27 2014

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]

AZD2281 is an experimental chemotherapeutic agent

3587 views | Feb 27 2014

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM [Read the Full Post]

E7080 is a multi kinase inhibitor that is being investigated for the treatment of various

3460 views | Feb 27 2014

E7080 (Lenvatinib) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β. Phase 3. [Read the Full Post]

BCL 2 inhibition with ABT 737 prolongs survival in an NRAS

2198 views | Feb 26 2014

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM [Read the Full Post]

Here we assess the in vitro and in vivo anti MM activity of MLN8237

2348 views | Feb 26 2014

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. [Read the Full Post]

PCI 24781 is a broad spectrum hydroxamic acid based inhibitor of HDAC

3582 views | Feb 25 2014

HDAC activity is measured using a continuous trypsin-coupled assay. [Read the Full Post]

Roscovitine is an experimental drug in the family

2009 views | Feb 25 2014

Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM. [Read the Full Post]

FTY720 is a first in class orally bioavailable

2223 views | Feb 24 2014

The inhibitory effect of S1P is revered by various concentrations of FTY720. [Read the Full Post]