Go6976

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Chemical Structure| 136194-77-9 同义名 : Gö 6976;PD406976
CAS号 : 136194-77-9
货号 : A494051
分子式 : C24H18N4O
纯度 : 99%+
分子量 : 378.426
MDL号 : MFCD00236434
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(132.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JAK2

  • PKCβ

    PKCβ1, IC50:6.2 nM

  • PKC

    PKC, IC50:7.9 nM

  • PKCα

    PKCα, IC50:2.3 nM

  • FLT3
描述 Go6976, a staurosporine analog, is an effective PKC inhibitor with an IC50 value of 20 nM[1]. Go6976 has been shown to eliminate S and G2 phase arrests. Dose-response experiments indicate that 30 nM of Go6976 can lift the S-phase arrest in 6 hours and the G2 arrest, leading to fatal mitosis after 24 hours. Treating cells with 100 nM Go6976 effectively removes S and G2 phase arrests at 6 and 24 hours, respectively, with a potency just marginally less than that of bovine serum. Cell viability is not reduced when treated with Go6976 alone, compared to the control at the utilized concentrations. When cytostasis is induced with SN38, the addition of 100 nM Go6976 to halted MDA-MB-231 cells leads to a significant reduction in the number of viable cells by 96 hours[2].
作用机制 Gö6976 is an ATP-competitive inhibitor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.21mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL
参考文献

[1]Qatsha KA, et al. Gö 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proc Natl Acad Sci U S A. 1993 May 15;90(10):4674-8.

[2]Hayamitsu Adachi, et al. Microbial metabolites and derivatives targeted at inflammation and bone diseases therapy: chemistry, biological activity and pharmacology. The Journal of Antibiotics volume 71, pages 60–71 (2018).