Remodelin
目录号 : GC11430
Remodelin 是 N-乙酰转移酶 10 (NAT10) 的小分子抑制剂。
Cas No.:1622921-15-6
Sample solution is provided at 25 µL, 10mM.
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Remodelin is a small molecule inhibitor of N-acetyltransferase 10 (NAT10).Dysregulation of N-acetyltransferase 10 (NAT10) is associated with the development of many types of tumors[1].
Combined remodelin and doxorubicin treatment reduced cell viability significantly more compared to cells treated with doxorubicin alone. EDU assays confirmed that both doxorubicin and remodelin decreased breast cancer cell proliferation more compared to cells treated with doxorubicin alone, suggesting remodelin attenuates doxorubicin resistance in breast cancer cells (MDA-MB-231)[2]
Remodelin was given daily by intragastric administration for 4 weeks. PDX model tumour volume was recorded and TGI was calculated. As a result, Remodelin significantly inhibited the growth of HNSCC PDXs in vivo[3]
The treatment of Remodelin could suppress the growth of cancer cells but not induce apoptosis, that Remodelin has little cytotoxicity. Remodelin significantly reduced AR-negative prostate cancer tumor growth. The anti-neoplastic effects of Remodelin through NAT10 inhibition should be credited to the slowing down of DNA replication, which could consequently attenuate replication stress-associated genomic instability, and ultimately delay the progression of prostate cancer[4]
References:
[1]. Ma R, Chen J, et al. Up regulation of NAT10 promotes metastasis of hepatocellular carcinoma cells through epithelial-to-mesenchymal transition.
[2]. Wu J, Zhu H, et al. Inhibition of N-acetyltransferase 10 using remodelin attenuates doxorubicin resistance by reversing the epithelial-mesenchymal transition in breast cancer. Am J Transl Res. 2018 Jan 15;10(1):256-264.
[3]. Tao W, Tian G, et al. NAT10 as a potential prognostic biomarker and therapeutic target for HNSCC. Cancer Cell Int. 2021 Aug 6;21(1):413.
[4]. Ma N, Liu H, et al.Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573.
Remodelin 是 N-乙酰转移酶 10 (NAT10) 的小分子抑制剂。N-乙酰转移酶 10 (NAT10) 的失调与多种肿瘤的发生有关[1]。
与单独使用多柔比星处理的细胞相比，重塑素和多柔比星联合处理显着降低了细胞活力。 EDU 测定证实，与单独使用阿霉素处理的细胞相比，多柔比星和重塑素都能更有效地降低乳腺癌细胞增殖，这表明重塑素可减弱乳腺癌细胞中的多柔比星耐药性 (MDA-MB-231)[2]
Remodelin 每天通过胃内给药给药，持续 4 周。记录PDX模型肿瘤体积并计算TGI。因此，Remodelin 在体内显着抑制 HNSCC PDXs 的生长[3]
Remodelin治疗可抑制癌细胞的生长但不诱导细胞凋亡，即Remodelin的细胞毒性很小。 Remodelin 显着降低了 AR 阴性前列腺癌肿瘤的生长。 Remodelin 通过抑制 NAT10 的抗肿瘤作用应归功于 DNA 复制的减慢，从而减弱复制应激相关的基因组不稳定性，并最终延缓前列腺癌的进展[4]
| Cell experiment [1]: | |
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Cell lines |
Mouse melanoma cell line(B16F10) |
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Preparation Method |
B16F10 cells were incubated with Remodelin and α- melanocyte - stimulating hormone (α-MSH) for 3 days. The harvested cells or media were centrifuged and the pellets were solubilized in sodium hydroxide for 1h. The melanin contents were measured using spectrophotometer at 475 nm wavelength (OD475). |
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Reaction Conditions |
10, 20 µM Remodelin for 3 days. |
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Applications |
α-MSH-mediated increase in the extracellular and intracellular melanin contents was significantly decreased upon treatment with 20 µM remodelin.Remodelin attenuates melanin synthesis by repressing MITF. |
| Animal experiment [2]: | |
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Animal models |
BALB/c nu/nu mice |
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Preparation Method |
AR-negative prostate Cancer Cells (PC-3 cells) were inoculated into the armpits of mice by subcutaneous injection. One week later, Remodelin injection was performed every two days for a total of 4 weeks. Tumor size was measured every two days. Tumors were excised from nude mice and weighed after 4 weeks. |
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Dosage form |
2,20 mg/kg Remodelin , i.p.injection |
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Applications |
Remodelin significantly reduced AR-negative prostate cancer tumor growth, and in the high-dose Remodelin group, xenograft tumor weight at the endpoint was also much smaller than that in the low-dose group.Remodelin suppresses the growth and tumorigenesis potential of prostate cancer cells. |
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References: [1]. Oh TI, Lee YM, et al.Inhibition of NAT10 Suppresses Melanogenesis and Melanoma Growth by Attenuating Microphthalmia-Associated Transcription Factor (MITF) Expression. Int J Mol Sci. 2017 Sep 7;18(9):1924. [2]. Ma N, Liu H, et al.Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573. |
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| Cas No. | 1622921-15-6 | SDF | |
| 化学名 | 4-[2-(2-cyclopentylidenehydrazinyl)-1,3-thiazol-4-yl]benzonitrile;hydrobromide | ||
| Canonical SMILES | C1CCC(=NNC2=NC(=CS2)C3=CC=C(C=C3)C#N)C1.Br | ||
| 分子式 | C15H15BrN4S | 分子量 | 363.28 |
| 溶解度 | ≥ 36.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7527 mL | 13.7635 mL | 27.527 mL |
| 5 mM | 0.5505 mL | 2.7527 mL | 5.5054 mL |
| 10 mM | 0.2753 mL | 1.3763 mL | 2.7527 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet