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Go 6983

CAS号

133053-19-7

分子式

C26H26N4O3

主要靶点

PKC

仅限科研使用

Cat No : CM06017

Print datasheet

Synonyms

inhibit|G? 6983|Go6983|Go-6983|Go 6983|Goe 6983|Goe6983|Goe-6983|Inhibitor|Protein kinase C|PKC|PKCα|PKCδ|PKCγ|PKCβ|PKCζ

验证数据展示

  • CAS No.: 133053-19-7

    Go 6983
    CAS#: 133053-19-7

产品信息

CAS号 133053-19-7
分子式 C26H26N4O3
主要靶点 PKC
主要通路 细胞骨架|表观遗传
分子量 442.51
纯度 99.04%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|G? 6983|Go6983|Go-6983|Go 6983|Goe 6983|Goe6983|Goe-6983|Inhibitor|Protein kinase C|PKC|PKCα|PKCδ|PKCγ|PKCβ|PKCζ

靶点活性

PKCβ:7 nM|PKCζ:60 nM|PKCα:7 nM|PKCδ:10 nM|PKCγ:6 nM

体内活性

Go 6983是靶向作用于ATP结合位点的亚型特异性PKC抑制剂。Go6983抑制ΔPfPKB活性,IC50为1 μM。1 μM Go6983与390 nM Ro-31-8425联用轻微抑制PGSMCs中Angiotensin II诱导的PLD2活性。在Go 6983（5 μM）处理的细胞中,下一个循环中的环数与对照培养物相比明显更少。 Go 6983（5 μM）处理导致恶性疟原虫培养物中新环形成减少近60％。300 μM Go6983抑制转染PKCμ的NIH3T3细胞中PKCμ自磷酸化降低20%。心脏再灌注PMNs和100 nM Go6983,左心室发展压和左心室发展压率分别恢复到基准值的89％和74％,明显高于PMNs单独处理。与心脏缺血再灌注（I/R）+ PMN 相比,100 nM Go6983 PMNs对内皮细胞的粘附和心肌浸润,并显著抑制了PMNs超氧化物释放90％。Go6983在PMNs存在时,降低I/R后心肌收缩功能障碍,这可能与降低超氧化物的产生相关。Go6983明显抑制先前对树花粉致敏的患者的抗原诱导的超氧化物从白细胞释放。Go6983抑制人类血管组织细胞内的Ca(2+)累积,说明其血管舒张特性机制。

体外活性

22.0 μg i.v. Go6983强烈抑制小鼠肺B16BL6肿瘤模型中51.2 %的肿瘤转移.

溶解度

DMSO:22.1 mg/mL (49.94 mM)

参考文献

1.Gschwendt M, et al. FEBS Lett, 1996, 392(2), 77-80.
2.Peterman EE, et al. J Cardiovasc Pharmacol, 2004, 43(5), 645-656.
3.Young LH, et al. Cardiovasc Drug Rev, 2005, 23(3), 255-272.
4.Andresen BT, et al. Hypertension, 2001, 37(2 Part 2), 635-639.
5.Kumar A, et al. J Biol Chem, 2004, 279(23), 24255-24264.
6.Zhang Y, Wang Z, Cao J, et al. Physiological crosstalk between the Mel1a and Mel1c pathways modulates melatonin-mediated, monochromatic light combination-induced bursa B-lymphocyte proliferation in chickens[J]. 2020
7.Zhang Y, Wang Z, Cao J, et al. A Green and Blue Monochromatic Light Combination Therapy Reduces Oxidative Stress and Enhances B-Lymphocyte Proliferation through Promoting Melatonin Secretion[J]. Oxidative Medicine and Cellular Longevity. 2021, 2021.
8.Fan Y L, Li B, Zhao H P, et al. A function of fascin1 in the colony formation of mouse embryonic stem cells[J]. STEM CELLS. 2020.

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