4829 Results for: "Adipogen"

Supplier: Adipogen

Polo-like kinase 1 (Plk1) is a regulator of the cell cycle that has been implicated in the pathology of many cancers. BI-2536 is a potent and selective small-molecule inhibitor of mammalian Plk1. It has inhibitory activity at subnanomolar concentrations and inhibits tumor growth in multiple tumor lines with IC(50) values below 1µM. BI-2536 also shows an 1,000-fold selectivity for PIK1 versus a large panel of other kinases. BI-2536 also demonstrated low Kd values against sister kinases PLK2 and PLK3. Preclinical studies in human cancer cell lines have shown that BI 2536 disrupts spindle assembly, resulting in mitotic arrest and inducing apoptosis. BI-2536 is currently in clinical trials against several types of solid tumor cancers.

Supplier: Adipogen

PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110delta-selective inhibitors that has been reported, with an IC(50) of 10nM.

Supplier: Adipogen

Pentoxifylline (PTX) metabolite. Can be used as reference material. Showed platelet aggregation in whole blood in vitro. Shown to be more effective than PTX in protecting WC/1 murine fibrosarcoma cells from TNF-alpha cytotoxicity and in inhibiting neutrophil superoxide anion production, degranulation (lactoferrin release) and surface expression of the beta-2 integrin CD11b/CD18.

Supplier: Adipogen

Bayer-18 is a selective TYK2 inhibitor, with an IC(50) of 18.7nM on TYK2 as measured by TYK2 HTRF assays. The compound shows 1000 fold selectivity against JAK2, CDK and KDR kinases in similar HTRF assays.

Supplier: Adipogen

Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5µM, respectively, and has shown favorable activity and tolerability in phase I and II trials in acute myeloid leukemia, with QT prolongation as the dose-limiting toxicity. Recently, AC220 has also been shown to be an effective inhibitor of ATP-binding cassette (ABC) proteins ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein). Quizartinib inhibited transport of fluorescent ABCG2 and ABCB1 substrates in ABCG2- and ABCB1-overexpressing cells in a concentration-dependent manner, from 0.1 to 5µM and from 0.5 to 10µM, respectively, and inhibited-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3µM, respectively.

Supplier: Adipogen

XL765 is active against class I PI3K (IC(50) = 39, 113, 9 and 43nM for p110alpha, beta, gamma and delta, respectively). XL765 also inhibits DNA-PK (IC(50) = 150nM) and mTOR (IC(50) = 157nM)

Supplier: Adipogen

Masitinib is a potent, orally available protein tyrosine kinase inhibitor targeting c-Kit, PDGFR and FGFR3. It demonstrates activity for Kit and PDGFRalpha/beta with IC(50) values of 200nM, 540nM and 800nM respectively. It shows weak inhibition of ABL and c-Fms.

Supplier: Adipogen

IC87114 is a potent, ATP-competitive, and selective inhibitor of PI3Kdelta. IC(50) values (130-500nM) for IC87114 are sub-micromolar over a wide range of ATP concentrations from 10µM to 200µM. IC87114 can selectively inhibit cellular migration but not adhesion as well as cellular polarization. More recent work has shown the PIK3delta inhibition also plays a role in autoimmune disease suppression.

Supplier: Adipogen

PIK-93 selectively inhibits the type III PI 4-kinase beta enzyme (IC(50) of 19nM). It has also been shown to have activity on PI3Kalpha with an IC(50) of 39nM.

Supplier: Adipogen

Genotoxic mycotoxin. Antitumor compound. Potent iNOS (NOSII) inhibitor. Interferes with cellular respiratory processes.

Supplier: Adipogen

Kinases, such as LIM kinase 1 (LIMK1) and LIM kinase 2 (LIMK2), have been identified as participating in signal pathways affecting actin dynamics by deactivating cofilin. Over expression of LMK1 has been found in invasive breast and prostate cancer cell lines and suppression of LIMK 2 expression has been found to limit migration of human fibrosarcoma cells. Thus, the inhibition of LIMK1 and/or LIMK2 enzymes have been suggested as targets for treating cancer, including reduction or prevention of metastasis. BMS-5 is a potent inhibitor of the LIM kinase. It has IC(50) values of 7nM and 8nM for LIMK1 and LIMK2 respectively. LIMK1/2 activity was measured via TCA precipitation assay using a biotinylated ADF (actin depolymization factor) as the protein substrate and the kinase domains of LIMK1 and LIMK2 as the enzyme sources in the presence of 1µM ATP.

Supplier: Adipogen

In recent years several groups have studied the sequence requirements, specificity, signaling pathways and kinetics of the TLR (Toll-like receptor) 9 suppression by inhibitory oligonucleotide motifs, which led to a class of novel inhibitory oligonucleotide (iODNs), that is independent of the previously thought species preference. Subsequently it has been discovered that telomeric DNA repeats (TTAGGG)n can block immune activation by CpG-ODNs. Short, 11-15 base long oligonucleotides were synthesized that were capable of potently inhibiting CpG-stimulation. The optimal inhibitory DNA motif consists of a pyrimidine-rich triplet, preferably CCT, which is positioned 5- to the GGG sequence in a singlestranded DNA molecule. Additionally, both the optimal spacing between the CCT and GGG motifs, as well as their relative order to each other, is of crucial importance for the inhibitory DNA action. Interestingly, although both TLR7/TLR8 ligands and bacterial DNA share the endosomal compartment for receptor binding and signal transduction, certain iODNs (G-type) suppress only TLR9-mediated activation, whereas prototype class I iODN may also interfere with the activation via the TLR7/TLR8 pathway. Recently, intriguing evidence has been presented that for some iODN classes the immuno-modulatory biological activity shows only limited sequence dependency or may not even involve TLR-mediated uptake and signaling pathways. For example iODNs of the class II are thought to act on immune activation through inhibition of STAT signaling and independent of TLR signaling via binding to a yet to be identified 'ODN-receptor'. Slightly modified phosphodiester versions of the most potent inhibitory ODNs were also able to profoundly block the immune activation of macrophages and just recently prove to be valuable tools for in vivo use in experimental animal models of inflammatory and auto-immune diseases. Based upon these recent insights the following classification for iODNs has been suggested: Class I: G-stretch ODNs: TLR9-specific competitors, some iODNs may also affect TLR7 and TLR8 signalingClass II: ODNs with telomeric repeats: TLR-independent inhibitors of STAT signaling (cellular uptake via an 'ODN receptor'?)Class III: Inhibitors of DNA uptake in a sequence independent mannerClass IV: Long phosphorothioate ODNs as direct competitors of TLR9 signaling in a sequence independent manner

Supplier: Adipogen

Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl, Lyn inhibitor with IC(50) values of 5.8nM and 19nM, respectively.

Supplier: Adipogen

AMG-1 is a potent inhibitor of human c-Met and RON with IC(50) values of 4 and 9nM respectively.

Supplier: Adipogen

Potent and selective protein kinase C (PKC) inhibitor. Inhibits panel of protein kinases (e.g. GSK-3beta, CDK2).

Supplier: Adipogen

Cell permeable superoxide dismutase (SOD) mimetic. Potent inhibitor of peroxynitrite-induced oxidative reactions (peroxynitrite scavenger), but not a scavenger of nitric oxide (NO). Neuronal apoptosis inhibitor. Protects T cells from superoxide generation, caspase-dependent DNA loss and cell death. Lipopolysaccharide-induced TNF-alpha production inhibitor, by prevention of intracellular ROS generation and subsequent inactivation of p38 MAPK and SAPK/JNK. .

Supplier: Adipogen

Nitric oxide (NO) donor. Generates both superoxide anion and nitric oxide that spontaneously form peroxynitrite. Platelet aggregation inhibitor. Guanylyl cyclase activator. Cytotoxic. Positive ionotropic. Vasodilator.

Supplier: Adipogen

Takeda-6d has potent inhibitory activity in both B-RAF with an IC(50) of 7.0nM and VEGFR2 with an IC(50) of 2.2nM.

Supplier: Adipogen

Phenoxy herbicide. Synthetic auxin. Compound can be used as analytical reference material.

Supplier: Adipogen

CYT387 is selective inhibitor of JAK1 and JAK2 kinases including the JAK2V617F mutant . Using ATP kinase assays IC(50) values for JAK1 (11nm), JAK2, (18nM), JAK2, JAK2V617F (23nM) JAK3 (155nM), and TYK2 (17nM). In testing kinase arrays, CYT387 also had activity (defined as an IC(50) 100nM) detected against CDK2/cyclin A, MAPK8 (JNK1), PRKCN (PKD3), PRKD1 (PKCµ), ROCK2, and TBK1 kinase as well.

Supplier: Adipogen

R406 is a strong Syk inhibitor with an IC(50) of 41nM. It inhibits Syk but not Lyn. It shows 5-fold less potency to Flt3.

Supplier: Adipogen

CD14/TLR4 antagonist. Inhibitor of sterile inflammation. Synthetic TLR4/CD14 ligand with TLR4 modulating activities in vitro, and conferring protection against TLR4/CD14-mediated tissue damage and inflammation in vivo. Useful to explore CD14- dependent and TLR4-independent pathways and TLR4 activation by endogenous ligands (e.g. hyaluronic acid oligosaccharides, oxLDL, HMGB1) in sterile inflammation. Shown to inhibit neuropathic pain, secondary necrosis of acute drug-induced liver failure and vascular inflammation, and abdominal aortic aneurysm by blocking non-hematopoietic TLR4 signaling. Useful tool, where inhibition of sterile (auto-) inflammation is desired, without compromising TLR4’s key role in the defense of pathogens.

Supplier: Adipogen

PI3Kgamma is required for for T-cell and B-cell as well as mast cell migration and degranulation. As such, these kinases are attractive targets for potential anti-infmamatory drugs. TASP0415914 has shown excellent results in cell based assays. It is orally available and has performed will in murine in vivo models. PI3Kgamma IC(50) 29nM, AKT IC(50) 294nM.

Supplier: Adipogen

NBD chloride is nonfluorescent until it reacts with primary or secondary amines to produce a fluorescent product. NBD chloride has been extensively used as a derivatizing reagent for chromatography analysis of amino acids and low molecular weight amines.

Supplier: Adipogen

Guanosine analog derivatized at position N7 and C8. Very potent immunostimulatory compound that increases cytokine production. Antitumor and antiviral activity compound. Potent and selective synthetic ligand for Toll-like receptor 7 (TLR7). Co-incubation with thymidine homopolymer oligodeoxynucleotides (ODN) redirected the stimulatory effect of loxoribine away from TLR7 toward TLR8. Induces autophagy and autophagy-induced cell death in Caco-2 cells. Shows adjuvant activity to increase the effectiveness of vaccines.

Supplier: Adipogen

Potent and selective cell permeable B-Raf (V600E) and c-Raf-1 (Y340D/Y341D) inhibitor. Antitumor compound. ERK phosphorylation is potently inhibited exclusive in B-Raf(V600E)-bearing tumor cell lines.

Supplier: Adipogen

Ca2+-indicator fluo-3 for use with visible-light excitation sources in flow cytometry and confocal laser-scanning microscopy. Since about 1996, fluo-3 has also been extensively used in cell-based high-throughput screening assays for drug discovery. Fluo-3 AM is essentially nonfluorescent until it is hydrolyzed intracellularly and/or in the presence of Ca2+. The green-fluorescent emission (~525 nm) of Ca2+-bound fluo-3 is conventionally detected using optical filter sets designed for fluorescein (FITC). As prepared by Minta, Kao and Tsien, fluo-3 was originally reported to undergo an ~40-fold increase in fluorescence upon binding Ca2+.

Supplier: Adipogen

Amidoxime fungicide used in agroculture. Active against powdery mildew of various crops in pre and post infection treatment. Has a long lasting translaminar and vapor phase activity. The mode of action is not know and it is considered different from that of other existing fungicides. It has favorable toxicological, ecotoxicological and environmental profiles. Compound can be used as analytical reference material.

Supplier: Adipogen

Tripyrrolic pigment like prodigiosin. Antimalarial agent. Anticancer agent with multiple modes of action. Immunosuppressant in non-toxic concentrations. Bone resorption inhibitor. Antiulcer agent.

Supplier: Adipogen

Cyanides/Nitriles. Organic building block for synthesis.