BMH-21
货号：
IB2330
品牌：
Jinpan
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产品简介
| EC | EINECS 809-833-1 |
| 别名 | N-[2-(二甲基氨基)乙基]-12-氧代-12H-苯并[G]吡啶并[2,1-B]喹唑啉-4-甲酰胺 |
| 英文名称 | BMH-21 |
| CAS | 896705-16-1 |
| 分子式 | C21H20N4O2 |
| 分子量 | 360.41 |
| 储存条件 | 2~8度 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | BMH-21是一种DNA嵌入剂，与核糖体DNA结合，并抑制RNA polymerase I (Pol I)转录。[1] |
| In Vitro | BMH-21引起RPA194蛋白酶体依赖性破坏，RPA194为Pol I全复合物的大催化亚基蛋白。[1]在U2OS癌症细胞系，BMH-21导致RPA194降解和NCL易位，IC50分别为0.05 μM 和 0.07 μM。通过引起核仁应激，BMH-21对细胞活性也表现出有效的抑制。[2] |
| In Vivo | 在小鼠异种移植物中，BMH-21降低肿瘤的生长。[1] |
| 激酶实验 | Cells were treated with BMH-21 for 3 hr and extracts were prepared in SB-buffer (20 mM HEPES pH 7.5, 1.5 mM MgCl2, 5 mM KCl, 1 mM dithiothreitol, protease inhibitors [Roche], 15 mM creatine phosphate, 2 mM ATP). Reactions were carried out in a mix containing human recombinant E1 (32 ng/ml), UbcH5c (50 ng/ml), UbcH10 (10 ng/ml), ubiquitin (50 ng/ml), Ub-aldehyde, and supplemented with 5 mM ATP. Reactions were initiated by addition of in vitro translated pRPA194-HA (TNT Coupled Reticulocyte Lysate System; Promega) and incubated for 90–120 min at 30_x005f C. MG132 was used at 85 mM when indicated.[1] |
| SMILES | O=C(C1=CC=CN2C1=NC3=C(C=C4C(C=CC=C4)=C3)C2=O)NCCN(C)C |
| 靶点 | DNA/RNA Synthesis |
| 动物实验 | For tumor xenograft experiments, A375 (3 x106) or HCT116 (2×106) cells were injected in 0.1 ml PBS to the flanks of 6-week-old athymic NCr nu/nu mice, and the tumors were allowed to establish until they reached 90–120 mm3. Mice were randomized to respective treatment groups (mock, BMH-21 25 mg/kg and BMH-21 50 mg/kg). Mock treatments consisted of phosphate-citrate buffer (pH 6.0). Treatments were administered intraperitoneally on a cycle 6 days on, 1 day off (A375) or daily (HCT116). Tumor weight (TW) was calculated by measuring the tumor diameter with a caliper and using the formula: TW = (L 3 W2)/2 where L is the tumor length and W is the tumor width. Tumor growth ratios were calculated as Dtumor weight(median) of treated group/Dtumor weight (median) control group.[1] |
| 数据来源文献 | [1] Peltonen K, et al. Cancer Cell. 2014, 25(1), 77-90. [2] Colis L, et al. J Med Chem. 2014, 57(11), 4950-4961. |
| 规格 | 5mg 10mg 25mg |
BMH-21是一新型DNA嵌入剂(DNA intercalator)，能结合rDNA并抑制RNA polymerase I的转录，不使组蛋白H2AX磷酸化。