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Blog of Signaling Pathways

SB939 is a novel histone deacetylase inhibitor with improved

3752 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

3464 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

3527 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

3448 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

2130 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

2987 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

2091 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

3588 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]

Adriamycin is an anti cancer chemotherapy drug

0 views | Jan 27 2014

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. [Read the Full Post]

Bortezomib is the first therapeutic proteasome inhibitor to be tested in humans

2857 views | Jan 26 2014

Bortezomib, a boronic acid dipeptide, is a highly selective, reversible inhibitor of the 26S proteasome which primarily functions in the degradation of mis-folded proteins and is essential for the regulation of the cell cycle. [Read the Full Post]

Nutlin 3 is a cis imidazoline analog

3777 views | Jan 26 2014

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]

Gsk256066 is a potent and selective inhaled PDE4 inhibitor

2344 views | Jan 24 2014

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. [Read the Full Post]

E7080 is a multi kinase inhibitor that is being investigated

2657 views | Jan 24 2014

E7080, as a potent inhibitor of in vitro angiogenesis, shows a significantly inhibitory effect on VEGF/KDR and SCF/Kit signaling. [Read the Full Post]

We describe the mechanism of action of WP1130

4674 views | Jan 22 2014

WP1130 (Degrasyn) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). [Read the Full Post]

MS 275 is a benzamide histone deacetylase inhibitor undergoing clinical trials

3734 views | Jan 22 2014

MS-275 shows inhibitory to HDACs by 2-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. [Read the Full Post]

MS 275 is a benzamide histone deacetylase inhibitor

3632 views | Jan 21 2014

MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5

0 views | Jan 21 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]

XL184 is currently undergoing clinical trials for the treatment of prostate

2650 views | Jan 21 2014

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [Read the Full Post]