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PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM.PF-3845 selectively inhibits FAAH by carbamylating FAAH¡¯s serine nucleophile.

June 21, 2017

prudect name : PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM.PF-3845 selectively inhibits FAAH by carbamylating FAAH¡¯s serine nucleophile.PF 3845 Synonyms: CAS NO: 1196109-52-0Molecular…

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PP2 is a substance that has frequently been used in cancer research as a “selective” inhibitor for Src-family kinases. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 µM) and JAK2 (50 µM). Despite its extensive use as a Src-selective inhibitor, recent research has shown that PP2 is non-selective and inhibits many other kinases with similar affinities.

prudect name : PP2 is a substance that has frequently been used in cancer research as a “selective” inhibitor for Src-family kinases. It strongly inhibits the kinases Lck (IC50=4 nM),…

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ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome. Recent evidence suggests that the immunoproteasome regulates the production of several inflammatory cytokines, including Tumor Necrosis Factor-¦Á (TNF-¦Á), Interleukin-6 (IL-6), IL-17, and IL-23. In preclinical models of rhematoid arthritis and lupus, ONX 0914 blocked progression of these diseases at well-tolerated doses. Preclinical studies are underway to evaluate the potential of ONX 0914 in the treatment of a range of autoimmune disorders.

prudect name : ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to…

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4-(3-((5-Ethynylpyridin-2-yl)oxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide

prudect name : 4-(3-((5-Ethynylpyridin-2-yl)oxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamidePF3845YNE Synonyms: CAS NO: 1196109-53-1Molecular Formula: C25H24N4O2Molecular Weight: 412.48Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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PCI-32765 is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.PCI-32765 is highly active and well tolerated in CLL/SLL pts irrespective of high risk genomic abnormalities. Although follow-up is short, the high response rate and very low progression rate suggests that PCI-32765 may be an important new targeted treatment approach for CLL pts. In ex vivo assays with whole bold, PCI-32765 prevents the activation of human BCR with an IC50 of about 0.2 ¦ÌM, while not influencing the activation of T cell. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-¦ÊB. In addition, PCI-32765 prevents activation-induced proliferation of CLL cells in vitro, and effectively inhibits survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-¦Á), fibronectin engagement, and stromal cell contact.

prudect name : PCI-32765 is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.PCI-32765 is highly active and well tolerated in CLL/SLL pts…

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Synonyms:4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide;PF 429242;o)Meth (2-MetR)-4-((diethylaMinyl)-Nhoxyphenethyl)-N-(pyrrolidin-3-yl)benzaMide;4-((diethylaMino)Methyl)-N-(2-Methoxyphenethyl)-N-(pyrrolidin-3-yl)benzaMide

prudect name : Synonyms:4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide;PF 429242;o)Meth (2-MetR)-4-((diethylaMinyl)-Nhoxyphenethyl)-N-(pyrrolidin-3-yl)benzaMide;4-((diethylaMino)Methyl)-N-(2-Methoxyphenethyl)-N-(pyrrolidin-3-yl)benzaMidePF 429242 Synonyms: CAS NO: 947303-87-9Molecular Formula: C25H35N3O2Molecular Weight: 409.56Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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PP242 is a novel potent and selective mTOR inhibitor with an IC50 of 8 nM. PP242 also shows residual (micromolar) activity against panel of tyrosine kinases. But PP242 was much less active against other PI3K family members with IC50 of 2, 2.2, 0.1, 1.3 and 0.41 ¦ÌM for p110¦Á, p110¦Â, p110¦Ä, p110¦Ã and DNA-PK, respectively. PP242 inhibits other PI 3-Kinases only at much higher concentrations. PP242, but not rapamycin, causes death of mouse and human leukemia cells. In vivo, PP242 delays leukemia onset and augments the effects of the current front-line tyrosine kinase inhibitors more effectively than does rapamycin. PP242 was also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma cells. In addition, PP242 was an effective agent against primary multiple myeloma cells in vitro and growth of 8226 cells in mice. Knockdown of the TORC2 complex protein, rictor, was deleterious to multiple myeloma cells further supporting TORC2 as the critical target for PP242.

prudect name : PP242 is a novel potent and selective mTOR inhibitor with an IC50 of 8 nM. PP242 also shows residual (micromolar) activity against panel of tyrosine kinases. But…

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RG3039, also known as PF-06687859, is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models.

prudect name : RG3039, also known as PF-06687859, is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion…

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Biological Activity:Potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM). Displays 50 – 250-fold selectivity over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro

prudect name : Biological Activity:Potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM). Displays 50 – 250-fold selectivity over other protein kinases. Blocks serum and fibronectin-directed…

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prudect name : P7C3-A20Synonyms: 3,6-Dibromo-beta-fluoro-N-(3-methoxyphenyl)-9H-carbazole-9-propanamineCAS NO: 1235481-90-9Molecular Formula: C22H19Br2FN2OMolecular Weight: 506.21Purity: 98% minSolubility: in DMSOStorage:

prudect name : P7C3-A20 Synonyms: 3,6-Dibromo-beta-fluoro-N-(3-methoxyphenyl)-9H-carbazole-9-propanamineCAS NO: 1235481-90-9Molecular Formula: C22H19Br2FN2OMolecular Weight: 506.21Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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