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SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $48 | In Stock | |
10 mg | $81 | In Stock | |
25 mg | $157 | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
Description | SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM). |
Targets&IC50 | ROCK1:56 nM, ROCK2:3 nM |
In vitro | 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. |
In vivo | 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. |
Kinase Assay | 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. |
Molecular Weight | 408.45 |
Formula | C22H24N4O4 |
Cas No. | 1072959-67-1 |
Smiles | CN(C)CCOc1cc(ccc1NC(=O)C1COc2ccccc2O1)-c1cn[nH]c1 |
Relative Density. | 1.298 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (97.93 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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