Blog of Signaling Pathways

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

2581 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

3311 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

4337 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

2678 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

2515 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

2490 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

4412 views | Dec 11 2013

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

R547 is a potent ATP competitive inhibitor of CDK

2620 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

3589 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

3310 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

2766 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

3811 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

2430 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

2741 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]

ABT 263 was formulated in 10 ethano

2839 views | Dec 05 2013

ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. [Read the Full Post]

BGB324 is a novel oral highly selective small molecule inhibitor

3533 views | Dec 05 2013

R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events [Read the Full Post]

Triciribine is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt

3645 views | Dec 04 2013

Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. [Read the Full Post]

Gefitinib is used to treat non small cell lung cancer in people

4485 views | Dec 04 2013

Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. [Read the Full Post]

LDN193189 is a cell permeable

3422 views | Dec 03 2013

LDN193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. [Read the Full Post]