| 中文名称: | Go6976 | ||||
|---|---|---|---|---|---|
| 英文名称: | Go6976 | ||||
| 别名: | 5,6,7,13-四氢-13-甲基-5-氧代-12H-吲哚并[2,3-A]吡咯并[3,4-C]咔唑-12-丙腈 5,6,7,13-Tetrahydro-13-Methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile | ||||
| CAS No: | 136194-77-9 | 分子式: | C24H18N4O | 分子量: | 378.43 |
| CAS No: | 136194-77-9 | ||||
| 分子式: | C24H18N4O | ||||
| 分子量: | 378.43 | ||||
基本信息
|
产品编号：G10434 |
|||||
|
产品名称：Go6976 |
|||||
|
CAS: |
136194-77-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
分子式： |
溶于液体 |
-80℃ |
六个月 |
||
|
分子量： |
378.43 |
-20℃ |
一个月 |
||
|
化学名： |
|
||||
|
Solubility (25°C) |
体外 |
DMSO |
44.7mg/mL warmed with 50ºC water bath (118.43mM) |
||
|
Ethanol |
Insoluble |
||||
|
Water |
Insoluble |
||||
|
体内（现配现用） |
0.5% CMC Na+1% Tween 80 |
30mg/mL |
|||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
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。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.6496mL |
13.2478mL |
26.4957mL |
|
5mM |
0.5299mL |
2.6496mL |
5.2991mL |
|
10mM |
0.2650mL |
1.3248mL |
2.6496mL |
|
50mM |
0.0530mL |
0.2650mL |
0.5299mL |
生物活性
|
产品描述 |
一种蛋白激酶C (PKC) 抑制剂，其 IC50 值为20nM。 |
||||
|
靶点/IC50 |
JAK2 |
FLT3 |
PKCα |
PKCβ1 |
PKC |
|
|
|
2.3nM |
6.2nM |
7.9nM |
|
|
体外研究 |
Go6976 is a potent inhibitor of PKC in vitro (IC50 is 20nM. This compound is structurally related to staurosporine, which is the most potent PKC inhibitor.UCN-01 is originally identified as a PKC inhibitor. Surprisingly, Go6976 is found to abrogate S and G2 arrest. Dose-response studies reveal that 30nM Go6976 is sufficient to cause abrogation of S-phase arrest in 6h and abrogation of G2 arrest followed by lethal mitosis in 24 h. Incubation of cells with 100nM Go6976 is sufficient to cause complete abrogation of S and G2 arrest at 6 and 24h, respectively, which is only slightly less potent than in bovine serum.Incubation of cells with UCN-01 or Go6976 alone do not decrease viability compared with control at the concentrations used. Incubation of cells with 5ng/mL SN38 result in cytostasis, and addition of 50nM UCN-01 or 100nM Go6976 to arrested MDA-MB-231 cells cause a dramatic decrease in viable cell number by 96h. |
||||
|
体内研究 |
Go6976 (2.5mg/kg i.p.)，作为PKD抑制剂，通过抑制MAPKs活化作用以减少TNF-α产生，而有效防止LPS/D:-GalN诱导的急性肝损伤，并显著提高LPS/D-GalN攻击的小鼠的存活率。 |
||||
推荐实验方法(仅供参考)
|
激酶实验： |
|
|
PKC 活性试验 |
简而言之，对于测量大鼠脑中的PKCαPKCβ1 和 PKC，200μl试验混合物包含50mM HEPES (pH7.5)，5mM MgCl2，1mM EDTA，1.25mM EGTA，1.32mM CaC12，1mM 二硫苏糖醇，1μg 磷脂酰丝氨酸，0.2μg 二油精，40μg 组蛋白Hi，10μM [γ-32P]ATP (1μCi/ml)，和5-10 单位 (pmol of Pi/min) PKC。加入[γ-32P]ATP开始测定，在30℃下培养5分钟，加入2ml 8.5% H3PO4停止测定，通过0.45-μm硝化纤维素过滤器过滤，并使用闪烁计数器进行评估。 |
|
细胞实验: |
|
|
Logarithmically growing cells are incubated with or without 5ng/mL SN38 for 24h and then incubated with or without 50nM UCN-01 or 100nM Go6976 for the following 24h. MDA-MB-231 (500 cells) or MCF-10A (1000 cells) are plated in 100μL in each well of a 96-well plate. The following day, drugs are added at the desired concentrations (Go6976: 1, 3, 10, 30, 100nM) and with the required schedule to replicate wells (a minimum of 4 wells/concentration). Drugs are removed, and plates are rinsed and then incubated for an additional 6 days. Inhibition of growth was then assessed on the basis of DNA content. Briefly, the media are removed, and attached cells are washed in 0.25×PBS, followed by the addition of 100μL of H2O. Cells are lysed by freeze/thawing the plates. Hoechst 33258 is added in high-salt buffer, cells are incubated for 2h,and fluorescence is measured. |
|
|
动物实验: |
|
|
动物模型 |
LPS/D-GalN-攻击的小鼠 |
|
剂量 |
2.5mg/kg |
|
给药处理 |
i.p. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
