Bryostatin 1(Synonyms: 苔藓抑素1)

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Bryostatin 1 (Synonyms: 苔藓抑素1) 纯度: ≥99.0%

Bryostatin 1 是一种天然的大环内酯类化合物,从苔藓虫 Bugula neritina 中分离出来,也是一种有效的中枢神经系统 (CNS) 渗透性的 PKC 调节剂。Bryostatin 1 以 Ki 值为 8.07 nM 和 0.45 nM 分别结合到分离的 Munc13-1 的 C1 域和全长的 Munc13-1 蛋白。Bryostatin 1 具有抗癌,抗炎,神经保护,抗 HIV-1 感染的特性。

Bryostatin 1(Synonyms: 苔藓抑素1)

Bryostatin 1 Chemical Structure

CAS No. : 83314-01-6

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生物活性

Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4].

IC50 & Target

PKC[1]
HIV-1[4]

体外研究
(In Vitro)

Bryostatin 1 (1 µM; 5 minutes; HT22 cells) treatment successfully recruits Munc13-1 from the cytosol to the plasma membrane. Effects of Bryostatin 1 on the other Munc13 family members, ubMunc13-2 and bMunc13-2, resembled those of Munc13-1 for translocation [1].
The increased level of expression of Munc13-1 following a 24 h incubation with Bryostatin 1 in both HT22 and primary mouse hippocampal cells is observed[1].
Bryostatin 1 can also affect the immune system by modulating dendritic cells (DCs) via toll-like receptor 4 (TLR4) through the MyD88-independent pathway, which favors an anti-inflammatory environment by inducing a type 2 phenotype that promotes the differentiation of CD4+ T-helper (Th) lymphocytes into Th2 versus Th1 effector cells[2].

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

Western Blot Analysis[1]

Cell Line: HT22 cells
Concentration: 1 µM
Incubation Time: 5 minutes
Result: Caused Munc13-1 to transfer to the membrane fraction.

体内研究
(In Vivo)

Bryostatin 1 (30 μg/kg; intraperitoneal injection; 3 d per week; for 2 weeks; C57BL/6J mice) treatment abolishes the onset of EAE[2].

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

Animal Model: Female C57BL/6J mice (8-12-week-old) with MOG35-55[2]
Dosage: 30 μg/kg
Administration: Intraperitoneal injection; 3 d per week; for 2 weeks
Result: Abolished the onset of experimental autoimmune encephalomyelitis (EAE).

Clinical Trial

分子量

905.03

Formula

C47H68O17

CAS 号

83314-01-6

中文名称

苔藓抑素1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Blanco FA, et al. Munc13 Is a Molecular Target of Bryostatin 1. Biochemistry. 2019 Jul 9;58(27):3016-3030.

    [2]. Kornberg MD, et al. Bryostatin-1 alleviates experimental multiple sclerosis. Proc Natl Acad Sci U S A. 2018 Feb 27;115(9):2186-2191.

    [3]. Zeng N, et al. Bryostatin 1 causes attenuation of TPA-mediated tumor promotion in mouse skin. Mol Med Rep. 2018 Jan;17(1):1077-1082.

    [4]. Proust A, et al. HIV-1 infection and latency-reversing agents bryostatin-1 and JQ1 disrupt amyloid beta homeostasis in human astrocytes. Glia. 2020 Apr 6.

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