Blog of Signaling Pathways

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

5521 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

2921 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

2438 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

6523 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

4005 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

3215 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

3241 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

3898 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

2876 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]

Y 27632 is a biochemical tool used in the study of the rho associated protein kinase

5608 views | Jan 10 2014

Y-27632 2HCl is a selective ROCK1 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]

VX 702 is A p38 MAP kinase inhibitor

2617 views | Jan 09 2014

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. [Read the Full Post]

Bortezomib is a highly selective reversible inhibitor of the 26S proteasome

3274 views | Jan 09 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]

XL147 is an orally available inhibitor of phosphoinositide 3 kinase

2002 views | Jan 08 2014

XL147 inhibits class I PI3K isoforms in an ATP-competitive manner. In a panel of HER2-overexpressing human breast cancer cell lines [Read the Full Post]

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

2662 views | Jan 08 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]

Roscovitine is an experimental drug candidate in the family

2607 views | Jan 07 2014

Roscovitine is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM. [Read the Full Post]

AZD6244 is not competitive with ATP and inactivates the ERK1

2368 views | Jan 07 2014

AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. [Read the Full Post]

Bafetinib is a second generation tyrosine kinase inhibitor

3858 views | Jan 06 2014

Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells [Read the Full Post]

AZD1080 is a selective orally active brain permeable GSK3 inhibitor

0 views | Jan 06 2014

AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. [Read the Full Post]

Tariquidar is a P glycoprotein inhibitor undergoing research

4481 views | Dec 30 2013

Tariquidar displays high-affinity binding to P-gp with Bmax of 275 pmol/mg. [Read the Full Post]