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ML327

ML327

产品编号 T4252   CAS 1883510-31-3

ML327 是 MYC 的阻断剂,还可抑制 E-钙粘蛋白转录和逆转上皮间质转化。

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ML327 Chemical Structure
ML327, CAS 1883510-31-3
规格 价格/CNY 货期 数量
1 mg ¥ 461 现货
5 mg ¥ 1,160 现货
10 mg ¥ 1,830 现货
25 mg ¥ 3,730 现货
50 mg ¥ 5,450 现货
100 mg ¥ 7,650 现货
1 mL * 10 mM (in DMSO) ¥ 1,280 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: ML327 (T4252)
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参考文献
产品描述 ML327 is a MYC blocker. ML327 can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
体外活性 ML327 partially restores E-cadherin expression at the plasma membrane in NMuMG cells induced to undergo Epithelial-to-Mesenchymal Transition (EMT) by TGF-β1 treatment. Treatment with ML327 induces an elongated morphology in neuroblastoma cells. BE(2)-C cells treated with ML327 demonstrates G1 cell cycle arrest with a concordant decrease in S phase population, and a significant increase in the sub G0 population. ML327 induces the expression of CDH1 in all seven of the neuroblastoma cell lines with a 50 to 1,400-fold induction of CDH1 mRNA expression. ML327 blocks the expression of MYC family of oncogenic transcription factors in all tested neuroblastoma cell lines. Immunoblotting time course demonstrates early repression of N-MYC expression within 2 h of treatment with ML327 (10 μM). p53 levels are also suppressed by treatment with ML327.
体内活性 ML327 treatment results in a two-fold decrease in MYCN expression, confirming that ML327 inhibits xenograft MYCN expression (p=0.0035). ML327 treatment significantly reduces tumor volume by three-fold over the two-week treatment period (p=0.02). Tumor explant weights are approximately three-fold smaller in the ML327-treated mice (p=0.01). Mice treated with ML327 lost 12% more body weight compared to vehicle-treated mice.
细胞实验 ML327 is solubilized in DMSO for in vitro experiments.Cells are seeded onto 96-well plates at equivalent density (3,000 to 10,000 depending upon cell line), permitted to attach overnight, and treated with either ML327 (10 μM) or vehicle. Daily absorbance measurements (450 nm) using the cell counting kit are obtained. For estimation of IC50 values, cells are plated at equal density, permitted to attach, and baseline absorbance is obtained using cell counting kit. Cells are then treated with varying doses of ML327 (0.1 to 30 μM) and cell viability is measured 72 h after treatment.
动物实验 ML327 is solubilized in 70% polyethylene glycol for in vivo experiments.Male athymic nude mice (4 to 6 weeks old) are maintained as described. BE(2)-C cells xenografts are established as previously described. 1×106 cells/100 μL of HBSS is injected subcutaneously into flanks using a 26-gauge needle (n=10 per group). Mice are monitored daily for xenograft formation and assessed by measuring the two greatest perpendicular tumor diameter with venier calipers. Xenograft volumes are estimated using the following formula [(length×width2)/2]. Once tumors reach 75 to 100 mm3, mice are randomized to receive either 50 mg/kg of ML327 or control vehicle (70% polyethylene glycol) via intraperitoneal injection twice daily for 14d. Weight and tumor volume are recorded daily. After completion of two weeks of treatment, mice are euthanized and tumors are excised, weighed, and RNA is isolated.
分子量 366.37
分子式 C19H18N4O4
CAS No. 1883510-31-3

存储

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

溶解度

DMSO: 13.75 mg/mL (37.53 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7295 mL 13.6474 mL 27.2948 mL 68.237 mL
5 mM 0.5459 mL 2.7295 mL 5.459 mL 13.6474 mL
10 mM 0.2729 mL 1.3647 mL 2.7295 mL 6.8237 mL
20 mM 0.1365 mL 0.6824 mL 1.3647 mL 3.4119 mL

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TargetMol Library Books参考文献

1. Rellinger EJ, et al. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Jul 20;8(53):91040-91051. 2. An H, et al. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.Oncotarget. 2015 Sep 8;6(26):22934-48.
CBP/p300-IN-2 MYCi361 Moracin D Moracin T VPC-70063 Mycro 3 Aaptamine Nicotinamide N-oxide

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 已知活性化合物库 Wnt/Hedgehog/Notch 通路化合物库 抗癌细胞代谢库 糖酵解化合物库 细胞凋亡化合物库 NO PAINS 化合物库 抗癌化合物库 细胞重编程化合物库

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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。

Keywords

ML327 1883510-31-3 Autophagy Cell Cycle/Checkpoint c-Myc Myc Inhibitor ML-327 inhibit ML 327 inhibitor

 

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