SR-3677
产品名称:SR-3677
产品描述:
产品描述 | SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM). |
靶点活性 | ROCK1:56 nM, ROCK2:3 nM |
体外活性 | SR-3677 has an IC50 of ~3 nM in enzyme and cell-based assays and has an off-target hit rate of 1.4% against 353 kinases, and inhibits only 3 out of 70 non-kinase enzymes and receptors. The IC50 value of SR-3677 for ROCK-I is 56 nM. |
体内活性 | SR-3677 increases ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 μM SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points. |
激酶实验 | 5 μL mixture of a 1 μM STK2 substrate and ATP (ROCK-I: 4 μM; ROCK-II: 20 μM) in STK-buffer is added to the wells. 20 nL of test compounds (SR-3677) is dispensed. The reaction is started by addition of 5 μL of 2.5 nM. ROCK-I or 0.5 nM ROCK-II in STK-buffer. After 4 h at RT, the reaction is stopped by the addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in the detection buffer. |
分子量 | 408.45 |
分子式 | C22H24N4O4 |
CAS No. | 1072959-67-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 40 mg/mL (97.93 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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