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Blog of Signaling Pathways

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

2317 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

3790 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

3617 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

2317 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

2355 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

2609 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

2287 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

5040 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

3212 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

3572 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

2378 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

1910 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

2296 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

2255 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]

This study is designed to evaluate the efficacy and safety of tofacitinib

6440 views | Oct 30 2013

Tofacitinib citrate inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. [Read the Full Post]

MK 8776 is a potent and functionally selective targeting cell

2542 views | Oct 30 2013

SCH 900776 is not a potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. [Read the Full Post]

IOX2 is a potent inhibitor of HIF 1 prolyl hydroxylase 2 with IC50

4216 views | Oct 29 2013

IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. [Read the Full Post]

PP242 is a new small molecule protein kinase inhibitor

2362 views | Oct 29 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]

VX809 is an experimental drug for the treatment of cystic fibrosis

2535 views | Oct 28 2013

VX-809 acts at the level of the ER to allow a fraction of the F508del-CFTR to adopt a properly folded form, to exit the ER and mobilize to the cell surface for normal functioning. [Read the Full Post]

Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma

1942 views | Oct 28 2013

In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. [Read the Full Post]