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Blog of Signaling Pathways

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

2056 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

2347 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

2376 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

2970 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

3121 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

3843 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

2909 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]

AZD6244 is a drug being investigated for the treatment of various types of cancer

0 views | Dec 03 2013

AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. [Read the Full Post]

Adriamycin is an anti cancer chemotherapy drug

2638 views | Dec 02 2013

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

Rapamycin is a bacterial macrolide with an tifungal

0 views | Dec 02 2013

Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. [Read the Full Post]

XL765 is an orally available inhibitor of PI3K

1641 views | Nov 29 2013

SAR245409 (XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM . [Read the Full Post]

Nutlin 3 inhibits the interaction between the proteins p53 and MDM2

3649 views | Nov 29 2013

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. [Read the Full Post]

BYL719 is an orally bioavailable phosphatidylinositol 3 kinase inhibitor

1833 views | Nov 28 2013

BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. [Read the Full Post]

PP242 hydrate for your research needs

1970 views | Nov 28 2013

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. [Read the Full Post]

Dapagliflozin is a drug used to treat type 2 diabetes

2342 views | Nov 27 2013

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. [Read the Full Post]

Dovitinib is a small molecule multitargeted receptor tyrosine kinase inhibitor

3620 views | Nov 27 2013

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 of 25 nM. [Read the Full Post]

Paclitaxel is a mitotic inhibitor used in cancer chemotherapy

1721 views | Nov 26 2013

Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. [Read the Full Post]

Bortezomib is the first therapeutic proteasome inhibitor

2848 views | Nov 26 2013

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. [Read the Full Post]

CUDC 101 is a potent inhibitor of histone deacetylase

3439 views | Nov 25 2013

CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. [Read the Full Post]

Cediranib is a potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases

2296 views | Nov 25 2013

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. [Read the Full Post]