PKA
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S2670 | A-674563 | 72 mg/mL | 72 mg/mL | 18 mg/mL |
| S1582 | H 89 2HCl | 6 mg/mL | 104 mg/mL | <1 mg/mL |
| S2554 | Daphnetin | <1 mg/mL | 35 mg/mL | <1 mg/mL |
| S7563 | AT13148 | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S7857 | 8-Bromo-cAMP | 80 mg/mL | 5 mg/mL | <1 mg/mL |
| S7858 | Dibutyryl-cAMP (Bucladesine) | 98 mg/mL | 98 mg/mL | 19 mg/mL |
PKA产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2670 |
A-674563A-674563是一种Akt抑制剂，在无细胞试验中Ki为11 nM，对PKA适度有效，作用于Akt1比作用于PKC选择性高30多倍。 |
Cell survival was determined using a WST-1 assay in the human lung cancer cells A549 A. and NCI-H358 B. following treatment with either an AKT1 specific inhibitor, A-674563 (black circle and line) or a pan-AKT inhibitor MK-2206 (gray square and line). *p < 0.05.
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| S1582 |
H 89 2HClH 89 2HCl是一种有效的PKA抑制剂，无细胞试验中Ki为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。 |
The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
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| S2554 |
DaphnetinDaphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。 |
C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
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| S7563 |
AT13148AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。 |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
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| S7857 |
8-Bromo-cAMP8-Bromo-cAMP是一种细胞渗透性环AMP(cAMP)类似物，激活cAMP依赖的蛋白激酶的Ka值为0.05 μM。是一种PKA激活剂。 |
(E) 8-Bromo-cAMP treatment could not restore the T cell defects in rpc9-/- mutants. |
|
| S7858 |
Dibutyryl-cAMP (Bucladesine)Dibutyryl-cAMP (Bucladesine)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2670 |
A-674563A-674563是一种Akt抑制剂，在无细胞试验中Ki为11 nM，对PKA适度有效，作用于Akt1比作用于PKC选择性高30多倍。 |
Cell survival was determined using a WST-1 assay in the human lung cancer cells A549 A. and NCI-H358 B. following treatment with either an AKT1 specific inhibitor, A-674563 (black circle and line) or a pan-AKT inhibitor MK-2206 (gray square and line). *p < 0.05.
|
|
| S1582 |
H 89 2HClH 89 2HCl是一种有效的PKA抑制剂，无细胞试验中Ki为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。 |
The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
|
|
| S2554 |
DaphnetinDaphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。 |
C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
|
|
| S7563 |
AT13148AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。 |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7857 |
8-Bromo-cAMP8-Bromo-cAMP是一种细胞渗透性环AMP(cAMP)类似物，激活cAMP依赖的蛋白激酶的Ka值为0.05 μM。是一种PKA激活剂。 |
2016, 143(12):2103-10 2018, 22(11):5518-5532 |
(E) 8-Bromo-cAMP treatment could not restore the T cell defects in rpc9-/- mutants. |
| S7858 |
Dibutyryl-cAMP (Bucladesine)Dibutyryl-cAMP (Bucladesine)是一种细胞可渗透性 PKA 激活剂，通过模拟内源性 cAMP 发挥作用。 |
2017, 7(6):1447-1462 |
