Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion[1][2].
IC50 & Target
Ki: 2.75 nM (protein kinase C)[1]
体外研究 (In Vitro)
Bryostatin 3 (1 μM; 24 h) does not inhibit [3Hlthymidine incorporation and largely blocks the growth-inhibitory action of TPA[2]. Bryostatin 3 (1 μM; 24 h) blocks the action of TPA to inhibit cell proliferation but does not block TPA-enhanced cell-substratum adhesion[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
888.99
Formula
C46H64O17
CAS 号
143370-84-7
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]. Wender PA, et, al. Modeling of the bryostatins to the phorbol ester pharmacophore on protein kinase C. Proc Natl Acad Sci U S A. 1988 Oct;85(19):7197-201.
[2]. Mackanos EA, et, al. Bryostatins selectively regulate protein kinase C-mediated effects on GH4 cell proliferation. J Biol Chem. 1991 Jun 15;266(17):11205-12.
Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion[1][2].
IC50 & Target
Ki: 2.75 nM (protein kinase C)[1]
体外研究 (In Vitro)
Bryostatin 3 (1 μM; 24 h) does not inhibit [3Hlthymidine incorporation and largely blocks the growth-inhibitory action of TPA[2]. Bryostatin 3 (1 μM; 24 h) blocks the action of TPA to inhibit cell proliferation but does not block TPA-enhanced cell-substratum adhesion[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
888.99
Formula
C46H64O17
CAS 号
143370-84-7
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]. Wender PA, et, al. Modeling of the bryostatins to the phorbol ester pharmacophore on protein kinase C. Proc Natl Acad Sci U S A. 1988 Oct;85(19):7197-201.
[2]. Mackanos EA, et, al. Bryostatins selectively regulate protein kinase C-mediated effects on GH4 cell proliferation. J Biol Chem. 1991 Jun 15;266(17):11205-12.
Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion[1][2].
IC50 & Target
Ki: 2.75 nM (protein kinase C)[1]
体外研究 (In Vitro)
Bryostatin 3 (1 μM; 24 h) does not inhibit [3Hlthymidine incorporation and largely blocks the growth-inhibitory action of TPA[2]. Bryostatin 3 (1 μM; 24 h) blocks the action of TPA to inhibit cell proliferation but does not block TPA-enhanced cell-substratum adhesion[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
888.99
Formula
C46H64O17
CAS 号
143370-84-7
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]. Wender PA, et, al. Modeling of the bryostatins to the phorbol ester pharmacophore on protein kinase C. Proc Natl Acad Sci U S A. 1988 Oct;85(19):7197-201.
[2]. Mackanos EA, et, al. Bryostatins selectively regulate protein kinase C-mediated effects on GH4 cell proliferation. J Biol Chem. 1991 Jun 15;266(17):11205-12.
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.
