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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
AZA1
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1071098-42-4
- 规格:
10mg/1mg/5mg
| 规格: | 10mg | 产品价格: | ¥4790.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥1190.0 |
| 规格: | 5mg | 产品价格: | ¥2990.0 |
| 基本信息 | |
| CAS | No.1071098-42-4 |
| 英文名称 | AZA1 |
| 分子式 | C22H20N6 |
| 分子量 | 368.43 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| SMILES | CC1=CC2=C(N1)C=CC(=C2)NC3=NC(=NC=C3)NC4=CC5=C(C=C4)NC(=C5)C |
| InChIKey | SYWHWWKOIJCMKF-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H20N6/c1-13-9-15-11-17(3-5-19(15)24-13)26-21-7-8-23-22(28-21)27-18-4-6-20-16(12-18)10-14(2)25-20/h3-12,24-25H,1-2H3,(H2,23,26,27,28) |
| PubChem CID | 25104141 |
| 靶点 | Rac1;Cdc42 |
| 通路 | Cell Cycle; GPCR & G Protein |
| 背景说明 | 是 Rac1 和 Cdc42 的有效抑制剂。 |
| 生物活性 | AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1, an inhibitor of Ras homolog oncoprotein (Rho) GTPase family proteins, RAS-related C3 botulinus toxin substrate 1 (Rac 1) and Cell division control protein 42 homolog (Cdc42) markedly inhibited cell invasion of galectin-1 and galectin-3 suggesting that Rac 1 and Cdc42 may be involved in the regulation of H-ALCL cell invasion of galectins[1-2]. |
| In Vitro | In androgen-independent prostate Cancer cells, AZA1 inhibited both Rac1 and Cdc42 but not RhoA GTPase activity in a dose-dependent manner and blocked cellular migration and proliferation. Cyclin D1 expression significantly decreased following Rac1/Cdc42 inhibition in prostate Cancer cells. AZA1 treatment also down-regulated PAK and Akt activity in prostate Cancer cells, associated with induction of the pro-apoptotic function of BAD by suppression of serine-112 phosphorylation.[1] |
| 细胞实验 | Daily systemic administration of AZA1 for 2 weeks reduced growth of human 22Rv1 prostate tumor xenografts in mice and improved the survival of tumor-bearing Animals significantly.[1] |
| 细胞实验 | AZA1 (Rac1/Cdc42-IN-1) (2-10 μM; 72 hours) blocks the proliferation of human prostate cancer cells 22Rv1 prostate cancer cells. AZA1 (2-10 μM; 24 hours) reduces phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells. AZA1 (10 μM; 24 hours) blocks Rac1 and Cdc42-dependent cell cycle events in 22Rv1 prostate cancer cells[1]. |
| 动物实验 | AZA1 (Rac1/Cdc42-IN-1) (100 μg; i.p.; daily for 2 weeks) is potent in suppressing human 22Rv1 xenograft growth in mice and improving survival[1]. |
| 数据来源文献 | [1]. Zins K, et al. A Rac1/Cdc42 GTPase-specific small molecule inhibitor suppresses growth of primary human prostate cancer xenografts and prolongs survival in mice. PLoS One. 2013;8(9):e74924. Published 2013 Sep 11. [2]. Suzuki O, et al. Sialylation and glycosylation modulate cell adhesion and invasion to extracellular matrix in human malignant lymphoma: Dependency on integrin and the Rho GTPase family. Int J Oncol. 2015;47(6):2091‐2099. |
| 单位 | 瓶 |
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文献和实验了样品的液流技术、细胞的分选和计数技术,以及数据的采集和分析技术等。 2.细胞的参量和荧光探针 FCM 是通过测量细胞的多种参量来获取信息的,细胞参数分为结构参量和功能参量两大类。结 构参量主要用于描述细胞的化学组分和形态特征,例如DNA、RNA的含量,总蛋白含量、胞内PH值 和细胞大小等;功能参量主要是描述细胞整体的理化和生物特性,如:细胞周期动力学、特殊配体的鉴 定、特殊细胞的生物活性等,这些参量有的需要经荧光标记才能被测定,有的并不需要荧光标记[4]。 2.1参数
氧化应激分子机制与相关信号通路:解码细胞 “氧化危机” 的底层逻辑
。 (三)MAPK 通路:氧化应激介导的 “细胞命运调节器” 通路核心分子:细胞外信号调节激酶(ERK)、c-Jun 氨基末端激酶(JNK)、p38 MAPK、MAPK 激酶(MKK)、转录因子 c-Jun/ATF2、凋亡蛋白 Bax/FasL。 通路工作机制:MAPK 通路包含 ERK、JNK、p38 三个功能差异化的亚家族,其激活依赖 MKK 的磷酸化级联反应。低浓度 ROS 可激活 ERK 通路,通过磷酸化下游靶蛋白推动细胞周期进展,促进细胞增殖;而高浓度 ROS 会抑制 ERK 活性,同时激活
2,3-DPG:2,3-diphosphatidylglyceric acid,2,3-二磷酸甘油酸 2-CdA:2-chlorodeoxyadenosin,cladribine,2-氯去氧腺苷 3H-TdR:tritiated thymide,氚标记胸腺嘧啶核苷 5-Aza:5-azacytidine,5-氮(杂)胞苷 a2-PI:a2-antiplasmin, a2-纤溶酶原抑制物 AA:aplastic anemia,再生障碍性贫血 AAV:adeno-associated
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