CaMK
- 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 | ||
| S7436 | NH125 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8274 | STO-609 | <1 mg/mL | 8 mg/mL | <1 mg/mL |
| S7423 | KN-93 Phosphate | 92 mg/mL | 100 mg/mL | <1 mg/mL |
| S7422 | KN-62 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8366 | CRT0066101 | 82 mg/mL | 25 mg/mL | 2 mg/mL |
| S7188 | CID755673 | <1 mg/mL | 43 mg/mL | <1 mg/mL |
| S3766 | Tanshinone IIA sulfonate (sodium) | -1 mg/mL | 79 mg/mL | -1 mg/mL |
特异性亚型抑制剂
- CaMK抑制剂（7）
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7436 |
NH125NH125 是一种选择性eEF-2 kinase抑制剂，IC50为60 nM,其选择性高于PKC, PKA和CaMKII 125倍 , 同时它也是强效的 histidine kinase 抑制剂。 |
NH125 sensitizes NPC cells to lapatinib. NPC cells were treated with lapatinib or DMSO for 48 h in the presence or absence of 0.25 μM NH125. Cell viability was assessed by the CCK-8 assay. Results are expressed as means±standard deviation. *, P<0.05;**, P<0.01 and ***, P<0.001.
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| S8274 |
STO-609STO-609是特异性的CaM-KK的抑制剂，抑制CaM-KKα和CaM-KKβ的活性，Ki值分别为80 ng/ml和15 ng/ml，并抑制其自身磷酸化活性。 |
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| S7423 |
KN-93 PhosphateKN-93 H3PO4 是一种强效的特异性的Ca2+/calmodulin-dependent protein kinase II (CaMKII)抑制剂，其 Ki 为 0.37 μM,对 APK, PKC, MLCK 或 Ca2+-PDE 没有明显的抑制活性。 |
Paeoniflorin (PF) protects the heart against MI-induced injury in DM mice. Heart function was analyzed by measuring fractional shortening {FS = [LV end diastolic diameter (LVEDD)-LVend systolic diameter (LVESD)]×100/LVEDD} and LV ejection fraction [LVEF = (LVEDD2−LVESD2)/LVEDD2].
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| S7422 |
KN-62KN-62是有效的、特异的CaMKⅡ抑制剂，Ki值为0.9 nM。同时也是一种非竞争性purinergic receptor P2RX7的拮抗剂（IC50=15 nM)。KN-62对CaMKⅡ是高选择性的，相对于对PKA、PKC和MLCK的选择性。同等抑制CaMKI和CaMKIV，抑制CaMK V的Ki值为0.8 μM。 |
(F) HEK239 cells were transfected with Flag-Cyclin D1 and Cyclin D1 siRNAs for 12 h, then cells were subjected to immunoblot detection. (G) DIV7 cortical neurons were treated with 10 μM KN62 or 15 μM Ntide and transfected with or without Cyclin D1 siRNAs for 24 h (Left panel), then apoptosis was determined. MW, molecular weight; kDa, kilodalton. All data in this figure represent the means ± SEM of three independent experiments. *P < 0.05.
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| S8366 |
CRT0066101CRT0066101是PKD (Protein Kinase D)家族的特异性小分子抑制剂，在杜仲癌细胞类型中（包括A549h和MiaPaCa-2细胞），特异地抑制PKD1/2/3的活性，而不影响PKCα/PKCβ/PKCε活性。对PKD1/2/3的IC50分别为1, 2.5, 2 nM。 |
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| S7188 |
CID755673CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂，IC50值分别为180 nM, 280nM,以及227 nM，选择性比其它CAMKs高大约200倍。 |
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| S3766 |
Tanshinone IIA sulfonate (sodium)Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen; a potent negative allosteric modulator of the human purinergic receptor P2X7. |
