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Blog of Signaling Pathways

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

3004 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

3947 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

2425 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

2769 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

4866 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

3930 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

3825 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

2799 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]

PLX4032 was able to reduce numbers of cancer cells

0 views | Jan 21 2014

Vemurafenib is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM. [Read the Full Post]

PCI 32765 is an anticancer drug targeting B cell malignancies

3628 views | Jan 20 2014

PCI-32765 shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. [Read the Full Post]

UNC0638 is an inhibitor of G9a and GLP with excellent potency and selectivity

2411 views | Jan 20 2014

UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. [Read the Full Post]

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

0 views | Jan 17 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]

Y 27632 is available in a 5 mg format and has been optimized

5029 views | Jan 17 2014

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. [Read the Full Post]

Abt 199 is designed to block the protein Bcl 2

2661 views | Jan 16 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]

R547 is a potent and selective ATP competitive CDK inhibitor

2223 views | Jan 16 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]

WP1066 is a cell permeable AG 490 tyrphostin analog

5974 views | Jan 15 2014

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. [Read the Full Post]

Bafetinib is a dual Bcr Abl and Lyn kinase inhibitor

3661 views | Jan 15 2014

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2. [Read the Full Post]

MLN9708 is a proteasome inhibitor and is the first to enter clinical trials as an oral preparation

2843 views | Jan 14 2014

MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. [Read the Full Post]

SP600125 is a reversible ATP competitive inhibitor

2871 views | Jan 14 2014

SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. [Read the Full Post]