- ￥351 - 3720
- TargetMol
- T6303L
- 2026年07月07日
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- 详细信息
- 文献和实验
- 技术资料
- CAS号：
2453324-32-6
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥783.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥351.0 |
| 规格： | 2mg | 产品价格： | ￥463.0 |
| 规格： | 5mg | 产品价格： | ￥632.0 |
| 规格： | 10mg | 产品价格： | ￥1032.0 |
| 规格： | 25mg | 产品价格： | ￥1744.0 |
| 规格： | 50mg | 产品价格： | ￥2600.0 |
| 规格： | 100mg | 产品价格： | ￥3720.0 |
Product Introduction
Bioactivity
| 名称 | CCT128930 hydrochloride |
| 描述 | CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM). |
| 体外活性 | In U87MG human glioblastoma cells, CCT128930 hydrochloride(0.1-60 μM; 1 hour) shows an initial induction of AKT phosphorylation at serine 473 up to 20 μM, followed by a decreased in phosphorylation at higher concentrations[1]. CCT128930 (18.9 μM) hydrochloride causes an increase in phosphorylation of pSer473 AKT after 30 minutes, which is sustained for 48 hours. Total AKT protein signal decreases gradually from 8 hours to 48 hours of treatment[1]. The GI50 values of CCT128930 hydrochloride for growth inhibition are 6.3 μM for U87MG human glioblastoma cells, 0.35 μM for LNCaP human prostate cancer cells, and 1.9 μM for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines[1]. CCT128930 hydrochloride inhibits direct substrates of AKT (Ser9 GSK3β, pThr246 PRAS40 and pT24 FOXO1/p32 FOXO3a) at ≥5 μM, and the downstream target, pSer235/236 S6RP at ≥10 μM, with generally constant levels of the respective total proteins and GAPDH[1]. |
| 体内活性 | CCT128930 hydrochloride shows antitumor activities in U87MG and BT474 human breast cancer xenografts[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 55 mg/mL (145.39 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.29 mM), Sonication is recommended. |
| 关键字 | U87MG | selective | PTEN | Protein kinase B | PKB | PKA | phosphorylation | p70S6K | Inhibitor | inhibit | growth | glioblastoma | DNA damage | cycle | cell | CCT-128930 Hydrochloride | CCT128930 hydrochloride | CCT-128930 | CCT128930 | CCT 128930 Hydrochloride | CCT 128930 | BT474 | breast cancer | Autophagy | arrest | Apoptosis | Akt2 | Akt |
| 相关产品 | Formamide | Urea | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Paeonol | Ethyl linoleate |
| 相关库 | Inhibitor Library | Angiogenesis related Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Colorectal Cancer Compound Library | Kinase Inhibitor Library | Anti-Aging Compound Library | Membrane Protein-targeted Compound Library | Immunology/Inflammation Compound Library | Tyrosine Kinase Inhibitor Library | PI3K-AKT-mTOR Compound Library |
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文献和实验Acids Glycine 75 50 0.667 L-Alanine 89 25 0.281 L-Arginine 211 105 0.498 L-Asparagine-H2O 150 50 0.333 L-Aspartic acid 133 30 0.226 L-Cysteine hydrochloride-H2O 176 100 0.568 L-Cystine 2HCl 313 31 0.0990 L-
Glutathione 还加入一定的L-Arginine-Hydrochloride 12-24h 4) 复性完毕在低浓度的缓冲液中连续缓慢透析12-24h 5) 复性率的测定 据变性蛋白和非变性蛋白的光学性质不同测定（望有经验的战友能更详细地讲解） 6）TritionX100、SDS这一类去垢剂最后不易去除，在制药行业中一般不允许采用。好像SDS最后残留量不能大于0.5%吧，忘了。 我用Triton洗涤有些包涵体效果不是很好。包涵体洗涤是纯化极为重要的一步，改变培养条件，再洗涤包涵体，有时可以在上柱前已经
加入适量Triton-X100. 2) 包含体溶解后装入透析袋在复性液中复性 3）复性液的组成很有讲究，本人使用 Oxidised Glutathione/ Reduced Glutathione 还加入一定的L-Arginine-Hydrochloride 12-24h 4) 复性完毕在低浓度的缓冲液中连续缓慢透析12-24h 5) 复性率的测定 据变性蛋白和非变性蛋白的光学性质不同测定（望有经验的战友能更详细地讲解） 6）TritionX100、SDS这一类去垢剂最后不易去除，在制药行业中
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