Blog of Signaling Pathways

E7080 is a multi kinase inhibitor that is being investigated

2783 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

4883 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

3949 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

3842 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

2814 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

3643 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

2426 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

5051 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

2677 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

2235 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

5999 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

3680 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

2857 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

2891 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]

OSI 930 is a novel inhibitor of the receptor tyrosine kinases Kit

0 views | Jan 13 2014

OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. [Read the Full Post]

AZD0530 is a dual specific inhibitor of Src and Abl

3594 views | Jan 13 2014

Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. [Read the Full Post]

Adriamycin is photosensitive and containers

2558 views | Jan 10 2014

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