Mezerein(Synonyms: 密执毒素;欧瑞香脂;)

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Mezerein (Synonyms: 密执毒素;欧瑞香脂;)

Mezerein 是一种 PKC 激活剂,具有抗白血病特性。 Mezerein 抑制表达 PKC alpha (IC50=1190 nM)、PKC beta1 (IC50=908 nM) 和 PKC delta (IC50=141 nM) 的酵母生长,但不抑制表达 PKC 的酵母生长。

Mezerein(Synonyms: 密执毒素;欧瑞香脂;)

Mezerein Chemical Structure

CAS No. : 34807-41-5

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生物活性

Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC[1][2].

体外研究
(In Vitro)

Mezerein is an antileukemic principle isolated from Daphne mezereum L[2].
Mezerein (50 ng/mL; 72 hours) potently inhibit tumorigenic murine macrophage cell line M5076 cellular proliferation[3].

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

Cell Proliferation Assay[3]

Cell Line: M5076 cells
Concentration: 50 ng/mL
Incubation Time: 72 hours
Result: Inhibited cellular proliferation (by greater than 90%).

体内研究
(In Vivo)

Mezerein exhibits antileukemic activity against the P-388 lymphocytic leukemia in mice. Mezerein (50 μg/kg) shows significant inhibitory activity against the P-388 and L-1210 leukemias in mice[2].

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

分子量

654.70

Formula

C38H38O10

CAS 号

34807-41-5

中文名称

密执毒素;欧瑞香脂;

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.

参考文献
  • [1]. L Saraiva, et al. Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta. Planta Med. 2001 Dec;67(9):787-90.

    [2]. S M Kupchan,et al.Mezerein: antileukemic principle isolated from Daphne mezereum L. Science. 1975 Feb 21;187(4177):652-3.

    [3]. N T Goode, et al. Protein kinase C-induced stimulation or inhibition of cellular proliferation in a murine macrophage tumor cell line. Cancer Res. 1990 Mar 15;50(6):1828-33.

PKC.beta.1(PRKCB1) 品牌:Carna Bio


PKC.beta.1(PRKCB1)

品牌:Carna Bio
CAS No.:
储存条件:-80℃
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(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

309-39731

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PKC.epsilon.(PRKCE) 品牌:Carna Bio


PKC.epsilon.(PRKCE)

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CAS No.:
储存条件:-80℃
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(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

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PKC.eta. 品牌:Carna Bio


PKC.eta.

品牌:Carna Bio
CAS No.:
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(生产商编号)

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PKC.theta.(PRKCQ) 品牌:Carna Bio


PKC.theta.(PRKCQ)

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* 干冰运输、大包装及大批量的产品需酌情添加运输费用


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Epsilon-V1-2(Synonyms: ε-V1-2 EAVSLKPT)

Epsilon-V1-2;(Synonyms: ε-V1-2; EAVSLKPT) 纯度: 98.18%

Epsilon-V1-2 (ε-V1-2) 是一种 PKCε 衍生肽,是一种选择性 PKCε 抑制剂。Epsilon-V1-2 抑制 PKCε 的转运,但不抑制 α-,β- 和 δPKC 的转运。

Epsilon-V1-2amp;;(Synonyms: ε-V1-2;  EAVSLKPT)

Epsilon-V1-2 Chemical Structure

CAS No. : 182683-50-7

规格 价格 是否有货 数量
5 mg ¥1800 In-stock
10 mg ¥3200 In-stock
25 mg ¥6400 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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Epsilon-V1-2 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • TGF-beta/Smad Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Cytoskeleton Compound Library
  • Peptide Library

生物活性

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC[1].

IC50 Target

PKCε

;

体外研究
(In Vitro)

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide containing the site for its specific receptor for activated C kinase (RACK), inhibits translocation of PKCε and reduces insulin response to glucose[1].
Epsilon-V1-2 (ε-V1-2; 1 µM, 24 hours) treatment significantly inhibits Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevents OA-induced gap junction disassembly in cardiomyocytes[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) treatment significantly improves the beating score in a murine heterotopic transplantation model. Epsilon-V1-2 reduces infiltration of macrophages and T cells into the cardiac grafts, and decreases parenchymal fibrosis. Epsilon-V1-2 treatment almost abolishes the rise in pro-fibrotic cytokine, TGF-β and monocyte recruiting chemokine MCP-1 levels[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice transplanted the hearts of FVB mice[3]
Dosage: 20 mg/kg/day
Administration: 0.1 mL osmotic pumps implanted subcutaneously; daily; for 4 weeks
Result: Significantly improved the beating score throughout the treatment.

分子量

843.96

Formula

C37H65N9O13

CAS 号

182683-50-7

Sequence Shortening

EAVSLKPT

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 50 mg/mL (59.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1849 mL 5.9245 mL 11.8489 mL
5 mM 0.2370 mL 1.1849 mL 2.3698 mL
10 mM 0.1185 mL 0.5924 mL 1.1849 mL

*

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, 6 months; -20°C, 1 month。-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。

参考文献
  • [1]. M Yedovitzky, et al. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20.

    [2]. Yuahn-Sieh Huang, et al. Mechanism of oleic acid-induced gap junctional disassembly in rat cardiomyocytes. J Mol Cell Cardiol. 2004 Sep;37(3):755-66.

    [3]. Tomoyoshi Koyanagi, et al. Pharmacological inhibition of epsilon PKC suppresses chronic inflammation in murine cardiac transplantation model. J Mol Cell Cardiol. 2007 Oct;43(4):517-22.

PKC.beta.1(PRKCB1) 品牌:Carna Bio


PKC.beta.1(PRKCB1)

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CAS No.:
储存条件:-80℃
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产品编号

(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

305-39733

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* 干冰运输、大包装及大批量的产品需酌情添加运输费用


* 零售价、促销产品折扣、运输费用、库存情况、产品及包装规格可能因各种原因有所变动,恕不另行通知,确切详情请联系上海金畔生物科技有限公司。

PKC.delta.(PRKCD) 品牌:Carna Bio


PKC.delta.(PRKCD)

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CAS No.:
储存条件:-80℃
纯度:
产品编号

(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

302-39743

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* 干冰运输、大包装及大批量的产品需酌情添加运输费用


* 零售价、促销产品折扣、运输费用、库存情况、产品及包装规格可能因各种原因有所变动,恕不另行通知,确切详情请联系上海金畔生物科技有限公司。

PKC.epsilon.(PRKCE) 品牌:Carna Bio


PKC.epsilon.(PRKCE)

品牌:Carna Bio
CAS No.:
储存条件:-80℃
纯度:
产品编号

(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

303-39751

100 ug 咨询


* 干冰运输、大包装及大批量的产品需酌情添加运输费用


* 零售价、促销产品折扣、运输费用、库存情况、产品及包装规格可能因各种原因有所变动,恕不另行通知,确切详情请联系上海金畔生物科技有限公司。

PKC.eta. 品牌:Carna Bio


PKC.eta.

品牌:Carna Bio
CAS No.:
储存条件:-80℃
纯度:
产品编号

(生产商编号)

等级 规格 运输包装 零售价(RMB) 库存情况 参考值

303-39773

5 ug 咨询


* 干冰运输、大包装及大批量的产品需酌情添加运输费用


* 零售价、促销产品折扣、运输费用、库存情况、产品及包装规格可能因各种原因有所变动,恕不另行通知,确切详情请联系上海金畔生物科技有限公司。