Blog of Signaling Pathways

The effect of panobinostat on HIV latency disruption in a phase 1/2 clinical trial

4881 views | Oct 22 2014

Rasmussen et al. found panobinostat, a histone deacetylase inhibitor, has the ability to activate infected cells from HIV latency. They also tested the safety of this strategy on phase 1/2 clinical trial. The effect of panobinostat treatment was not significant in reducing the number of latently infected cells. However, panobinostat effectively disrupt HIV latency in vivo. [Read the Full Post]

TIPE3, a new transfer protein of lipid second messengers regulates human cancer

2210 views | Oct 21 2014

Svethlana et al. found one of the transfer protein, TIPE3 (TNFAIP8L3), acts as a controller of phosphoinositide second messenger that promotes cancer. IPE3 may represent a valuable target in therapeutic treatment of malignant diseases. [Read the Full Post]

Two side roads toward conquest of HBV

2511 views | May 05 2014

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM. [Read the Full Post]

Copper dependent Cancer

1967 views | Apr 15 2014

Wortmannin is a PI3K with IC50 of 3 nM, first described PI3K inhibitors [Read the Full Post]

How to survive the zombie apocalypse

2388 views | Apr 02 2014

LDE225 (NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. [Read the Full Post]

Is it really that nonselective inhibitors have no future in clinical study

2191 views | Apr 01 2014

R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. [Read the Full Post]

Story of Bcr Abl continues

2262 views | Mar 28 2014

PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. [Read the Full Post]

Not all DUBs are equal

3439 views | Mar 21 2014

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. [Read the Full Post]

A small molecule bidentate binding dual inhibitor probe of the LRRK2 and JNK kinases

2145 views | Mar 17 2014

PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class

3014 views | Mar 13 2014

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]

Endocrine therapy has become the most important systemic treatment

4260 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

3157 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

3894 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

3778 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

3452 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

5128 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

2988 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

2054 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

2103 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]