Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PYZD-4409 是一种特异性 UBA1 抑制剂,IC50 为 20 μM。 PYZD-4409 在恶性细胞中诱导细胞死亡,并且对恶性细胞的细胞毒性优于对正常造血细胞的细胞毒性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 791 | 现货 | ||
5 mg | ¥ 1,830 | 现货 | ||
10 mg | ¥ 2,920 | 现货 | ||
25 mg | ¥ 4,830 | 现货 | ||
50 mg | ¥ 6,880 | 现货 | ||
100 mg | ¥ 9,290 | 现货 | ||
500 mg | ¥ 18,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,850 | 现货 |
产品描述 | PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells over normal hematopoietic cells. |
靶点活性 | Ubiquitin-activating enzyme UBA1:20 μM |
体外活性 | PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells. PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress and the unfolded protein response. PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34. PYZD-4409 (0-25 μM; 24 hours; K562 leukemia cells) significantly increases both mRNA and protein levels of Grp78 and Hsp70. PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells) induces cell death with an LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. Solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM [1]. |
体内活性 | PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) reduces tumor weight and volume[1]. |
分子量 | 351.67 |
分子式 | C14H7ClFN3O5 |
CAS No. | 423148-78-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35 mg/mL (99.53 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8436 mL | 14.2179 mL | 28.4357 mL | 71.0894 mL |
5 mM | 0.5687 mL | 2.8436 mL | 5.6871 mL | 14.2179 mL | |
10 mM | 0.2844 mL | 1.4218 mL | 2.8436 mL | 7.1089 mL | |
20 mM | 0.1422 mL | 0.7109 mL | 1.4218 mL | 3.5545 mL | |
50 mM | 0.0569 mL | 0.2844 mL | 0.5687 mL | 1.4218 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PYZD-4409 423148-78-1 Others Ubiquitination E1/E2/E3 Enzyme PYZD4409 Inhibitor E3 ligating enzyme E2 conjugating enzyme inhibit Ubiquitin activating enzyme E1 activating enzyme Ubiquitin ligase Ubiquitin conjugating enzyme PYZD 4409 inhibitor