手霉素A Manumycin A

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Manumycin A手霉素A                              Manumycin A

手霉素A



手霉素A                              Manumycin A



产品规格/储存说明


产品详情

产品类型:生化试剂



产品特性


分子式:C31H38N2O7

分子量:550.6

CAS52665-74-4

来源:从海洋放线菌(Streptomyces parvulus)中分离

纯度:≥98%(HPLC)

外观:黄色~棕色粉末

溶解性:溶于DMSO或甲醇,不溶于水

检测方式:1H-NMR检测

InChi KeyTWWQHCKLTXDWBD-MVTGTTCWSA-N

Smiles

CCCC[C@@H](C)C=C(/C)C=C(/C)C(=O)NC1=C[C@@](O)(C=CC=CC=CC(=O)NC2=C(O)CCC2=O)[C@@H]2O[C@@H]2C1=O

 


运输/储存条件


运    输:干冰运输

短期储存温度:+4°C

长期储存温度:-20°C

建议储存条件:避光

使用事项/稳定性:自生产后在-20°C下至少可稳定储存1年;溶解后避光储存于-20°C下。


◆产品应用


● 抗生素。

● 凋亡和内质网应激介导的细胞死亡诱导剂。

● 高效、高选择性、高竞争性的细胞渗透性ras法尼基转移酶(rasfarnesyltransferase抑制剂(IC50=30 nM )。

● 不影响香叶基香叶基转移酶(IC50 = 180 µM)。

● 对法尼基焦磷酸具有竞争性抑制作用,而对Ras的抑制作用为非竞争性。

● 中性鞘磷脂酶抑制剂。

● 阻断大鼠心肌细胞中胰岛素诱导的MAP激酶的激活(19 μM)。

● 靶向蛋白磷酸酶1α(PP1α),并还原过氧化氢。

● 纠正强直性肌营养不良1型(DM1)中肌肉氯离子通道Clcn1的异常剪接。

● 表现出潜在的抗炎活性。

● 不可逆的人硫氧还蛋白还原酶1(TrxR-1)抑制剂(IC50=272 nM)和NADPH氧化酶活性诱导剂。其很可能充当TrxR-1 C端氧化还原中亲核

● Sec残基的Michael受体,并产生SecTRAP(硒损害硫氧还蛋白还原酶来源凋亡蛋白),该蛋白通过氧化应激同时促进细胞凋亡、坏死,增加细

● 胞内活性氧(ROS)的产生。

● 由于外泌体释放过程中有Ras的参与,证实了手霉素A是一种外泌体分泌的抑制剂。

● 可治疗强直性肌营养不良1型(DM1)。

● 通过靶向蛋白磷酸酶1α 介导淋巴瘤细胞凋亡。

产品列表

产品编号

产品名称

包装

BVT-0091-M001

Manumycin A
手霉素A

1 mg

BVT-0091-M005

5 mg

BVT-0091-M010

10 mg

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参考文献


1.

Identification of Rasfarnesyltransferase inhibitors by microbial screening: M. Hara et al.; PNAS 90, 2281 (1993)

2.

Inhibitors of Rasfarnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review)

3.

Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994)

4.

Protein kinase C, but not tyrosine kinases or Ras, plays a critical role in angiotensin II-induced activation of Raf-1 kinase and extracellular signal-regulated protein kinases in cardiac myocytes: Y. Zou et al.; J. Biol. Chem. 271, 33592 (1996)

5.

Manumycin inhibits ras signal transduction pathway and induces apoptosis in COLO320-DM human colon tumour cells: A. Di Paolo, et al.; Br. J. Cancer 82, 905 (2000)

6.

Manumycin A and its analogues are irreversible inhibitors of neutral sphingomyelinase: C. Arenz, et al.; ChemBioChem 2, 141 (2001)

7.

Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells: M. She, et al.; Leukemia 19, 595 (2005)

8.

Binding of manumycin A inhibits IkappaB kinase beta activity: M. Bernier, et al.; J. Biol. Chem. 281, 2551 (2006)

9.

A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics: G. Porcu, et al.; Mol. Cancer 9:197 (2010)

10.

Targeting farnesyl-transferase as a novel therapeutcstrategy for mevalonate kinase defiency: In vitro and in vivo approaches: L. De Leo, et al.; Pharmacol. Res. 61, 506 (2010)

11.

Manumycin A corrects aberrant splicing of Clcn1 in myotonic dystrophy type 1 (DM1) mice: K. Oana, et al.; Sci. Rep. 3, 2142 (2013)

12.

Manumycin induces apoptosis in prostate cancer cells: J.G. Li, et al., Onco Targets Ther. 7, 771 (2014)

13.

The natural tumorcide Manumycin-A targets protein phosphatase 1α and reduces hydrogen peroxide to induce lymphoma apoptosis. G.B. Carey, et al.; Exp. Cell. Res. 332, 136 (2015)

14.

Manumycin A from a new streptomyces strain induces endoplasmic reticulum stress-mediated cell death through specificity protein 1 signaling in human oral squamous cell carcinoma: C.J. Jae, et al.; Int. J. Oncol. 47, 1954 (2015)

15.

Manumycin A downregulates release of proinflammatory cytokines from TNF alpha stimulated human monocytes: E. Cecrdlova, et al.; Immunol. Lett. 169, 8 (2016)

16.

Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration-resistant prostate cancer cells: A. Datta, et al.; Cancer Lett. 408, 73 (2017)

17.

Manumycin A Is a Potent Inhibitor of Mammalian Thioredoxin Reductase-1 (TrxR-1): A. Tuladhar & K.S. Rein; ACS Med. Chem. Lett. 9, 318 (2018)

18.

The free fatty acid receptor 1 promotes airway smooth muscle cell proliferation through MEK/ERK and PI3K/Akt signaling pathways: A. Matoba, et al.; Am. J. Physiol. 314, 333 (2018)

19.

Effectors of thioredoxin reductase: Brevetoxins and manumycin-A: A. Tuladhar, et al.; Comp. Biochem. Physiol. C Toxicol. Pharmacol. 217, 76 (2019)

20.

Inhibiting extracellular vesicles formation and release: a review of EV inhibitors: M. Catalano & L. O'Driscoll; J. Etracell. Vesicles 9, 1703244 (2020)

21.

Combination of photoactive hypericin and Manumycin A exerts multiple anticancer effects on oxaliplatin-resistant colorectal cells: M. Macejova, et al.; Toxicol. Vitro 66, 104860 (2020)

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