化合物VER-49009 T2268

Product Introduction
Bioactivity


英文名: VER49009

描述: VER49009 (CCT0129397) 是一种有效的 HSP90 抑制剂（IC50 =25 nM，Kd=78 nM）。

细胞实验: Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. (Only for Reference)

激酶实验: Fluorescence Polarization Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.

体外活性: 在人卵巢肿瘤模型中,腹腔注射VER-49009（4 mg/kg）能够诱导HSP90与ERBB2的解离.在无胸腺的小鼠中,静脉注射VER-49009（20 mg/kg ）能够发挥有效作用.

体内活性: VER-49009能够诱导HSP72和HSP27与与其结合蛋白解离,导致细胞周期停滞。在重组的酵母Hsp90蛋白中（IC50=167 nM）,VER-49009能够抑制內源性ATP酶活性。在肝纤维化的治疗中,VER-49009能够诱导肝细胞CFSC在G2期停滞积累,抑制细胞生长。

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

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 71 mg/mL (183.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: VER49009 | CCT 0129397 | CCT-0129397

相关产品: DTHIB | Luminespib | CH5138303 | Apoptozole | p5 Ligand for Dnak and DnaJ acetate | HSP90-IN-22 | Palmitic acid | NMS-E973 | DDO-5936 | Feretoside

相关库: HIF-1 Signaling Pathway Compound Library | Anti-Breast Cancer Compound Library | Oxidation-Reduction Compound Library | Endoplasmic Reticulum Stress Compound Library | CNS-Penetrant Compound Library | Apoptosis 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