Blog of Signaling Pathways

Deforolimus is a small molecule inhibitor of the mammalian target of rapamycin

2364 views | Dec 19 2013

Ridaforolimus is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. [Read the Full Post]

Wnt C59 was first disclosed in patent WO2010101849 as a potent

4065 views | Dec 19 2013

Wnt-C59 is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. [Read the Full Post]

Tipifarnib is a farnesyltransferase inhibitor

2760 views | Dec 18 2013

Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. [Read the Full Post]

AZD0530 is a dually active inhibitor of c Src and Bcr ABL

3313 views | Dec 18 2013

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). [Read the Full Post]

Givinostat is a histone deacetylase inhibitor with potential

3878 views | Dec 17 2013

Givinostat (ITF2357) is a potent HDAC inhibitor for HDAC2, HDAC1B and HDAC1A with IC50 of 10 nM, 7.5 nM and 16 nM. [Read the Full Post]

Abt199 is designed to block the function of the protein Bcl 2

2557 views | Dec 17 2013

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]

Bortezomib is the first clinically approved proteasome inhibitor for treating multiple human malignancies

3269 views | Dec 16 2013

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]

LY335979 is a potent inhibitor that contains a cyclopropyldibenzosuberane moiety

4310 views | Dec 16 2013

LY335979 competitively inhibits equilibrium binding of vinblastine to Pgp by blocking azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. [Read the Full Post]

AT101 was developed to put requirements in place for CPAs

2646 views | Dec 13 2013

AT-101 inhibits a panel of different lymphoproliferative malignancies with IC50 ranged from 1.2 μM to 7.4 μM. [Read the Full Post]

Pki587 is a highly potent dual PI3K kinase inhibitor

2486 views | Dec 13 2013

PKI-587 shows potent inhibitory activity against PI3K-α, PI3K-γ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. [Read the Full Post]

Olaparib is an experimental chemotherapeutic agent

0 views | Dec 12 2013

Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. [Read the Full Post]

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

2471 views | Dec 12 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]

XAV 939 is a small molecule and selective Wnt pathway

4335 views | Dec 11 2013

XAV-939 specifically inhibits tankyrase PARP activity. [Read the Full Post]

R547 is a potent ATP competitive inhibitor of CDK

2602 views | Dec 10 2013

R547 identified as a diaminopyrimidine compound, which is a potent and selective ATP-competitive CDK inhibitor. [Read the Full Post]

SB 525334 is a selective inhibitor of transforming growth factor B

3533 views | Dec 10 2013

SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. [Read the Full Post]

Salubrinal is a drug which acts as a specific inhibitor of eIF2a

3242 views | Dec 11 2013

Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). [Read the Full Post]

VX 770 is a drug approved for patients with a certain mutation of cystic fibrosis

2639 views | Dec 09 2013

Ivacaftor (VX-770, Kalydeco) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. [Read the Full Post]

Tandutinib is a small molecule inhibitor of the type

3780 views | Dec 09 2013

Tandutinib has little activity against EGFR, FGFR, KDR, InsR, Src, Abl, PKC, PKA and MAPKs. [Read the Full Post]

MP 470 is a potent and multi targeted inhibitor of c Kit

2387 views | Dec 06 2013

In mice xenograft models of HT-29, A549, and SB-CL2 cells, MP-470 (10 mg/kg–75 mg/kg via i.p. or 50 mg/kg–200 mg/kg via p.o.) inhibits tumor growth. [Read the Full Post]

EPZ005687 is the catalytic subunit of the polycomb repressive complex 2

2669 views | Dec 06 2013

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. [Read the Full Post]