普乐沙福 T1776

Product Introduction
Bioactivity


英文名: Plerixafor

描述: Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂，可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂，是免疫刺激剂和造血干细胞动员剂，还抑制HIV-1和HIV-2的复制，EC50为 1-10 nM。

细胞实验: Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2]. U87 mg cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous "Treatments" section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2].

激酶实验: In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively.

体外活性: Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]

体内活性: A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: PBS : 1 mg/mL (1.98 mM)
Ethanol : 50 mg/mL
DMSO : < 1mg/ml (insoluble）
H2O : Insoluble


关键字: JM 3100 | stream | inhibit | multiple | Inhibitor | SID-791 | Human immunodeficiency virus | Plerixafor | cancer | G-CSF | human | JM-3100 | stem | myeloma | SID 791 | cells | blood | CXC chemokine receptors | lymphoma | AMD3100 | SID791 | HIV | ligand | AMD 3329 | AMD3329 | mobilizer | CXCR | peripheral | AMD-3100

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相关库: Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Macrocyclic Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Obesity Compound Library | Anti-Cancer Active Compound Library | Anti-Viral Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途