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Blog of Signaling Pathways

MLN9708 is a proteasome inhibitor and is the first to enter clinical trials

3382 views | Feb 19 2014

MLN9708 is a selective, orally bioavailable, second-generation proteasome inhibitor. [Read the Full Post]

Cediranib is currently in double blind studies for the treatment

3534 views | Feb 18 2014

Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM [Read the Full Post]

ARQ197 is a staurosporine derivative that binds to the dephosphorylated MET kinase

2600 views | Feb 18 2014

Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM, little activity to Ron, and no inhibition to EGFR. [Read the Full Post]

Abt199 is designed to block the function of the protein Bcl2

2652 views | Feb 14 2014

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]

XL184 is a small molecule inhibitor of the tyrosine kinases

3264 views | Feb 14 2014

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM [Read the Full Post]

SB431542 is a small molecule that acts as a specific inhibitor

3705 views | Feb 13 2014

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases. [Read the Full Post]

RO4929097 is a small molecule gamma secretase inhibitor

3346 views | Feb 13 2014

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. [Read the Full Post]

SB525334 is a potent and selective inhibitor of TGFB

3561 views | Feb 12 2014

SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. [Read the Full Post]

TAK 875 was dissolved in dimethyl sulfoxide

2554 views | Feb 12 2014

AK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. [Read the Full Post]

Torin 1 is a potent and selective inhibitors of mTOR

2087 views | Feb 11 2014

Torin1 inhibits phosphorylation of mTORC1 and mTORC2 substrates in cells at concentrations of 2 and 10 nM, respectively. [Read the Full Post]

SB939 is a novel histone deacetylase inhibitor with improved

3946 views | Feb 11 2014

SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. [Read the Full Post]

Cediranib is a potent inhibitor of vascular endothelial growth factor

3640 views | Feb 10 2014

Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. [Read the Full Post]

Bosutinib is a tyrosine kinase inhibitor undergoing research

3733 views | Feb 10 2014

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM, respectively. [Read the Full Post]

Dasatinib is being evaluated for use in numerous other cancers

3610 views | Feb 08 2014

Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants. [Read the Full Post]

We describe the mechanism of action of WP1130

0 views | Feb 08 2014

WP1130 is a selective deubiquitinase inhibitor. [Read the Full Post]

BKM120 is a potent and cell permeable inhibitor of the PI3 kinase family

2249 views | Feb 07 2014

BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. [Read the Full Post]

GDC 0068 is a highly selective small molecule inhibitor of Akt

3119 views | Feb 07 2014

GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. [Read the Full Post]

MP 470 is a potent and multi targeted inhibitor

2203 views | Jan 29 2014

Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. [Read the Full Post]

BKM 120 is a drug that may slow the growth of cancer cells

0 views | Jan 29 2014

BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. [Read the Full Post]

Tariquidar is a P glycoprotein inhibitor undergoing research

3870 views | Jan 27 2014

Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM, reverses drug resistance in MDR cell Lines. [Read the Full Post]