标签归档：manzamine

Manzamine A (Synonyms: Keramamine A)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Manzamine A  (Synonyms: Keramamine A)

Manzamine A 是一种口服活性 β-carboline 生物碱，抑制 GSK-3β 和 CDK-5 的 IC50 值为 10.2 μM 和 1.5 μM。Manzamine A 靶向胰腺癌细胞的 vacuolar ATPases 并抑制自噬 (autophagy)。Manzamine A 具有抗疟和抗癌活性。Manzamine A 对 HSV-1 具有较强的活性。

Manzamine A (Synonyms: Keramamine A)

Manzamine A Chemical Structure

CAS No. : 104196-68-1

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Manzamine A 相关产品

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生物活性

Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4].

IC50 & Target[1][2][3]

Plasmodium

 

GSK-3β

10.2 μM (IC50)

CDK5

1.5 μM (IC50)

vacuolar ATPases

 

Malaria

 

HSV-1

 

体外研究
(In Vitro)

Manzamine A (5-50 µM, 18 h) decreases tau phosphorylation, measured with ELISA[1].
Manzamine A (10 µM) inhibits yeast S. cerevisiae growth by 30%[2].
Manzamine A displays a few enlarged vacuoles in yeast[2].
Manzamine A (2.5-10 µM, 24 h) increases acidity in pancreatic cancer cells and non-malignant Vero cells[2].
Manzamine A (1 µM, 24 h) inhibits HSV-1 infection in SIRC cells[4].
Manzamine A shows antimalarial activity with an IC50 of 8.0 nM (D6 clone) and 11 nM (W2 clone)[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Manzamine A 相关抗体:

Cell Viability Assay[4]

Cell Line: SIRC cell
Concentration: 0.1, 0.5, 1, 2, 3, 5, and 10 µM
Incubation Time: 72 h
Result: Inhibited SIRC cell viability with an IC50 of 5.6 µM.

体内研究
(In Vivo)

Manzamine A (50 and 100 mol/kg, p.o. or i.p.) inhibits the growth of the rodent malaria parasite Plasmodium berghei in infected mice[6].
Manzamine A (8 mg/kg, i.p., daily for 8 consecutive days) prolongs the survival of SW mice to 20 days[7].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Plasmodium berghei in infected mice[6]
Dosage: 50 or 100 mol/kg
Administration: Intraperitoneal injection (i.p.) or oral administration (p.o.)
Result: Inhibited the growth of the rodent malaria parasite Plasmodium berghei.
Prolonged the survival of highly parasitaemic mice.

分子量

548.76

Formula

C36H44N4O
CAS 号

104196-68-1
结构分类
  • Alkaloids
初始来源
  • 海洋天然产物
  • 海绵
  • 动物

Okinawan marine sponge
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 10 mg/mL (18.22 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8223 mL 9.1115 mL 18.2229 mL
5 mM 0.3645 mL 1.8223 mL 3.6446 mL
10 mM 0.1822 mL 0.9111 mL 1.8223 mL

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纯度 & 产品资料
Data Sheet (605 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Hamann M, et al. Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer’s disease. J Nat Prod. 2007;70(9):1397-1405.  [Content Brief]

    [2]. Kallifatidis G, et al. The marine natural product manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells [published correction appears in Mar Drugs. 2014;12(4):2305-7]. Mar Drugs. 2013;11(9):3500-3516. Published 2013 Sep 17.  [Content Brief]

    [3]. Winkler JD, et al. Antimalarial activity of a new family of analogues of manzamine A. Org Lett. 2006;8(12):2591-2594.  [Content Brief]

    [4]. Palem JR, et al. Manzamine A as a novel inhibitor of herpes simplex virus type-1 replication in cultured corneal cells. Planta Med. 2011;77(1):46-51.  [Content Brief]

    [5]. Wahba AE, et al. Structure-activity relationship studies of manzamine A: amidation of positions 6 and 8 of the beta-carboline moiety. Bioorg Med Chem. 2009 Nov 15;17(22):7775-82.  [Content Brief]

    [6]. Donia M, et al. Marine natural products and their potential applications as anti-infective agents. Lancet Infect Dis. 2003 Jun;3(6):338-48.  [Content Brief]

    [7]. El Sayed KA, et al. New manzamine alkaloids with potent activity against infectious diseases. J Am Chem Soc. 2001 Mar 7;123(9):1804-8.  [Content Brief]

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