Archive for June 2017

Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively.

 June 21, 2017

prudect name : Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with…

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SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 ¦ÌM. SB 525334 blocks phosphorylation induced by TGF-¦Â1 and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB 525334 also inhibits the increased mRNA expression levels of plasminogen activator inhibitor-1 (PAI-1) and procollagen ¦Á1(I) induced by TGF-¦Â1 in A498 renal epithelial carcinoma cells at 1 ¦ÌM).SB 525334 (1 ¦ÌM) attenuates the heightened sensitivity to TGF-¦Â1 exhibited by pulmonary artery smooth muscle cells (PASMCs) from patients with familial forms of idiopathic pulmonary arterial hypertension (PAH).

prudect name : SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 ¦ÌM. SB 525334 blocks phosphorylation induced by TGF-¦Â1 and nuclear…

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prudect name : SC-144Synonyms: CAS NO: 895158-95-9Molecular Formula: Molecular Weight: Purity: 98% minSolubility: In DMSOStorage:

prudect name : SC-144 Synonyms: CAS NO: 895158-95-9Molecular Formula: Molecular Weight: Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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SB505124 is identified as a reversible ATP competitive and selective ALK inhibitor of ALK4 and ALK5. SB505124 shows no toxicity to renal epithelial A498 cells at concentrations up to 100 ¦ÌM for 48 hours, and blocks TGF-¦Â¨Cinduced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner. In human umbilical vein endothelial cells (HUVEC), SB505124 (500 nM) blocks the changes of TGF-¦Â1 on F-actin assembly and prevents ROS production induced by TGF-¦Â. By inhibiting TGF-beta1 signaling, SB505124 leads to decreased deferoxamine (DFO)-induced neurogenesis. A recent study shows that SB505124 suppresses the migration and invasion of breast cancer MCF-7-M5 cells.

prudect name : SB505124 is identified as a reversible ATP competitive and selective ALK inhibitor of ALK4 and ALK5. SB505124 shows no toxicity to renal epithelial A498 cells at concentrations…

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Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit ¦Á (eIF2¦Á). Salubrinal inhibited ER stress-mediated apoptosis induced by the protein glycosylation inhibitor tunicamycin (Tm) in a dose-dependent manner, with a median effective concentration (EC50) ∼ 15 ¦ÌM. Salubrinal also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, Salubrinal is not a general apoptosis inhibitor. Salubrinal induced rapid and robust eIF2¦Á phosphorylation and its downstream effects in PC12 cells, including down-regulation of cyclin D1 and up-regulation of GADD34 and CHOP, two proteins whose expression is induced by eIF2¦Á phosphorylation. Salubrinal inhibits eIF2¦Á dephosphorylation by inhibiting the PP1/GADD34 complex. Salubrinal inhibits HSV replication with IC50 of ~ 3¦ÌM by inhibiting eIF2¦Á dephosphorylation. Salubrinal increased non-rapid eye movement (NREM) sleep.

prudect name : Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit ¦Á (eIF2¦Á). Salubrinal inhibited ER stress-mediated apoptosis induced by the protein…

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Sitagliptin phosphate tablets is the first approved DPP-4 inhibitor, in type 2 diabetics Insulin by slowing incretin hormones play a role in the inactivation

prudect name : Sitagliptin phosphate tablets is the first approved DPP-4 inhibitor, in type 2 diabetics Insulin by slowing incretin hormones play a role in the inactivationSitagliptin phosphate monohydrate Synonyms:…

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S1RA(E-52862) is a potent and selective sigma-1 receptor(¦Ò1R, Ki=17 nM) antagonist, showed good selectivity against ¦Ò2R (Ki > 1000 nM).

prudect name : S1RA(E-52862) is a potent and selective sigma-1 receptor(¦Ò1R, Ki=17 nM) antagonist, showed good selectivity against ¦Ò2R (Ki > 1000 nM).S1RA(E-52862) Synonyms: CAS NO: 878141-96-9Molecular Formula: C20H23N3O2Molecular Weight:…

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Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.

prudect name : Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in…

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Saracatinib is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib exerts its activity through ATP competitive and reversible inhibition of the target enzyme. [1]Saracatinib potently inhibited the in vitro proliferation of Src3T3 mouse fibroblasts and demonstrated variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib(tumor types: colon, prostate, lung, and leukemia) was observed with IC50 values of 0.2¨C0.7 µM. In 3-day MTS cell proliferation assays, AZD0530 inhibited in vitro proliferation of the Bcr¨CAbl-driven human leukemia cell line K562 with an IC50 of 0.22 µM.In a head-to-head assay measuring EGFR phosphorylation in KB cells, Saracatinib exhibited an IC50 of 1.25 mM compared with 11 nM for gefitinib.

prudect name : Saracatinib is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib exerts…

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Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells (FLT3-WT), addition of FL was necessary to stimulate FLT3 phosphorylation, and treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high and low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand (FL), consistent with expression of FLT3-ITD. Sunitinib Malate (Sutent, SU11248) inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib (Sutent) to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib (Sutent) on ligand-dependent proliferation of cells was examined. Sunitinib (Sutent) inhibited VEGF- and FGF-induced proliferation of HUVECs with IC50 of 0.04 and 0.7 µM, respectively. Sunitinib (Sutent) also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFR¦Á or PDGFR¦Â with IC50 of 0.03 and 0.07 µM, respectively.

prudect name : Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells…

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