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Blog of Signaling Pathways

R428 inhibits angiogenesis in corneal micropocket and tumor models

3986 views | Nov 13 2013

R428 is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 and InsR, EGFR, HER2, and PDGFRβ. [Read the Full Post]

BMS 790052 is the most potent hepatitis C virus inhibitor

3771 views | Nov 13 2013

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. [Read the Full Post]

FK866 has been shown to induce apoptosis by non competitive

2673 views | Nov 12 2013

APO866 effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM. Phase 1/2. [Read the Full Post]

Rapamycin is a bacterial macrolide with an tifungal

2061 views | Nov 12 2013

Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM. [Read the Full Post]

AZD1080 is a selective orally active brain permeable GSK3 inhibitor

3839 views | Nov 11 2013

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against cdk2, cdk5, cdk1 and Erk2. [Read the Full Post]

Dasatinib is a novel potent and multi targeted inhibitor

2518 views | Nov 11 2013

Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. [Read the Full Post]

OSI 930 is an inhibitor of the receptor tyrosine kinases c Kit

2301 views | Nov 08 2013

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]

BMN 673 was generally well tolerated

3760 views | Nov 08 2013

BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. [Read the Full Post]

Olaparib is an experimental chemotherapeutic agent

3589 views | Nov 07 2013

Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). [Read the Full Post]

Nilotinib is a tyrosine kinase inhibitor approved for the treatment of chronic myelogenous leukemia

2303 views | Nov 07 2013

Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. [Read the Full Post]

WP1130 is a novel selective small molecular deubiquitinase

2331 views | Nov 06 2013

Administration of WP1130 inhibits the growth of K562 tumors as well as both wildtype Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. [Read the Full Post]

RAF265 Inhibits the Growth of Advanced Human Melanoma Tumors

2595 views | Nov 06 2013

RAF265 inhibits C-Raf, wild type B-Raf and mutant (V600E) B-Raf. RAF265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. [Read the Full Post]

FTY720 is a first in class orally bioavailable compound

2265 views | Nov 05 2013

The inhibitory effect of S1P is revered by various concentrations of FTY720, with IC50 effect of 173 nM. [Read the Full Post]

Thiazovivin is a drug which dramatically improves the survival of hES

5013 views | Nov 05 2013

Thiazovivin (Tzv) is a novel ROCK inhibitor with IC50 of 0.5 μM, promotes hESC survival after single-cell dissociation. [Read the Full Post]

BMN 673 is an orally bioavailable inhibitor of the nuclear

3191 views | Nov 04 2013

BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. [Read the Full Post]

SB939 is a pan histone deacetylase inhibitor binding

3537 views | Nov 04 2013

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

XL184 is a small molecule inhibitor of the tyrosine kinases c Met

2362 views | Nov 01 2013

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]

IPA 3 is a selective cell permeable Pak1 inhibitor

1898 views | Nov 01 2013

IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of IPA-3. [Read the Full Post]

Torin 1 is a potent and selective inhibitor of mTOR

2282 views | Oct 31 2013

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

Nilotinib is indicated for the treatment of adult patients

2234 views | Oct 31 2013

Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression. [Read the Full Post]