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Blog of Signaling Pathways

BYL719 is an orally bioavailable phosphatidylinositol 3 kinase inhibitor

1873 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

2018 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

2389 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

3699 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

1764 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

2922 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

3520 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

2348 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]

Decitabine is a drug for the treatment of myelodysplastic syndromes

2577 views | Nov 22 2013

Decitabine is a potent inhibitor of DNA methylation with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively. [Read the Full Post]

Thiazovivin helps in promoting human embryonic stem cell

4768 views | Nov 22 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]

AG 014699 is a PARP inhibitor being investigated as a potential anti cancer agent

3887 views | Nov 21 2013

Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. [Read the Full Post]

Roscovitine is a cell permeable reversible selective inhibitor

2393 views | Nov 21 2013

Roscovitine (Seliciclib, CYC202) 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. It shows little effect on CDK4/6. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5

3070 views | Nov 20 2013

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

PLX4032 was able to reduce numbers of cancer cells

2300 views | Nov 20 2013

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM. [Read the Full Post]

PD184352 is an inhibitor of mitogen activated protein kinase

2086 views | Nov 19 2013

CI-1040 (PD 184352) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM, 100-fold more selective for MEK1/2 than MEK5. Phase 2. [Read the Full Post]

Roscovitine is an experimental drug candidate in the family of pharmacological

2578 views | Nov 19 2013

Roscovitine (Seliciclib, CYC202) 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. It shows little effect on CDK4/6. [Read the Full Post]

NVP BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM

2575 views | Nov 18 2013

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition . [Read the Full Post]

ABT 199 is designed to block the function of the protein Bcl 2

2946 views | Nov 18 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]

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

2061 views | Nov 15 2013

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

PD 0325901 is a selective and ATP non competitive MEK inhibitor

2130 views | Nov 15 2013

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 1/2. [Read the Full Post]