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- CAS号：
866405-64-3
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1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥182.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥370.0 |
| 规格： | 10mg | 产品价格： | ￥552.0 |
| 规格： | 25mg | 产品价格： | ￥1144.0 |
| 规格： | 50mg | 产品价格： | ￥2064.0 |
| 规格： | 100mg | 产品价格： | ￥2344.0 |
| 规格： | 200mg | 产品价格： | ￥3432.0 |
Product Introduction
Bioactivity
| 名称 | Dorsomorphin |
| 描述 | Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity. |
| 细胞实验 | Dorsomorphin is dissolved in DMSO (10 mM) and stored,and then diluted with appropriate media (DMSO 0.5%) before use[2].HeLa and 786-O cells are treated with various concentrations of Dorsomorphin (0,0.3,1,3,10 μM ),Versipelostatin and Phenformin in the presence or absence of 10 mM 2DG or 1 μg/mL of Tunicamycin as a stressor for 30 h in 96-well plates.For the combination study,786-O cells are treated with various concentrations of UPR inhibitors in the presence or absence of 10 mM 2DG for 24 h.The medium is then replaced with fresh growth medium,and cells are cultured for a further 15 h.Subsequently,MTT is added to the culture medium,and the absorbance of each well is determined.For the viability assay under glucose-withdrawal conditions,HT1080 cells are treated with various concentrations of Dorsomorphin and phenformin in 12-well plates in the presence or absence of glucose for 18 h,seeded in 96-well plates with growth medium,and then cultured for a further 48 h before MTT is added.Relative cell survival (mean±SD of quadruplicate determinations) is calculated by setting each control absorbance from untreated cells as 100%.The effects of drug combinations at concentrations producing 80% cell growth inhibition (IC80) are analyzed using the isobologram method[2]. |
| 激酶实验 | HT1080 cells are seeded in 24-well plates (2×104 cells per well) and treated with Dorsomorphin in the presence or absence of glucose or 10 mM 2DG for 2 h. HT1080 cells that overexpressed the wild-type and dominant negative AMPKα1 are prepared by transfecting plasmid DNA (pAMPKα1-wt, pAMPKα1-D168A and pcFlag as a control) in 6-well plates, seeding in 24-well plate and treating with UPR inhibitors. Cells are lysed with cell lysis buffer (20 mM Tris-HCl, pH 7.5, 250 mM NaCl, 10% glycerol, 0.5% NP-40, 1 mM EDTA, 1 mM EGTA, 0.2 mM PMSF, 1 μg/mL pepstatin, 0.5 μg/mL leupeptin, 5 mM NaF, 2 mM Na3Vo4, 2 mM β-glycerophosphate, 1 mM DTT). Relative AMPK kinase activity (mean±SD of duplicate determinations) to control sample (vehicle or pcFlag under normal growth conditions) is determined using the CycLex AMPK kinase assay kit[2]. |
| 体外活性 | 方法：人肿瘤细胞 HeLa 和 HCT116 用 Dorsomorphin (1.25-80 μM) 处理 24 h，使用 CCK-8 方法检测细胞活力。 结果：Dorsomorphin 抑制 HeLa 和 HCT116 细胞的活力，IC50 值分别为 10.71 μM 和 11.34 μM。[1] 方法：ATL 患者来源的 PBMCs 细胞用 Dorsomorphin (5-25 μM) 处理 24 h，使用 Flow Cytometry 检测细胞凋亡情况。 结果：Dorsomorphin 以剂量依赖的方式增加了急性和慢性型 ATL 患者 PBMC 中早期凋亡细胞的频率。[2] |
| 体内活性 | 方法：为检测体内抗肿瘤活性，将 Dorsomorphin (10 mg/kg) 腹腔注射给携带人类肿瘤 S1T 的 NOD/SCID 小鼠，每天一次，持续二十八天。 结果：Dorsomorphin 抑制了 NOD/SCID 小鼠中人 ATL 肿瘤异种移植物的生长。[2] 方法：为检测体内对 SMAD 活性的影响，将 Dorsomorphin (10 mg/kg) 单次腹腔注射给 iron-dextran 处理的 C57BL/6 小鼠。 结果：Dorsomorphin 消除了 iron-dextran 引起的铁介导的肝脏 SMAD1/5/8 磷酸化的增加。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : 0.13 mg/mL (0.33 mM), Solution. DMSO : 1.33 mg/mL (3.33 mM), Sonication and heating are recommended. 1M HCI : 255 mg/mL (638.31 mM) |
| 关键字 | type | Transforming growth factor beta receptors | TGF-β/Smad | TGF-β Receptor | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | receptors | Inhibitor | inhibit | Dorsomorphin | BMP | BML275 | BML 275 | Autophagy | ATP-competitive | AMPK | AMP-activated protein kinase |
| 相关产品 | Chitosan oligosaccharide | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Autophagy Compound Library | Anti-Colorectal Cancer Compound Library | Kinase Inhibitor Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | NO PAINS Compound Library | TGF-beta/Smad Compound Library | Membrane Protein-targeted Compound Library | Immunology/Inflammation Compound Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 Dorsomorphin【866405-64-3】
￥182 - 3432
