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Home > Inhibitors & Agonists > Cell Cycle/DNA Damage > ROCK

SR3677

  Cat. No.:  DC7246   Featured
Chemical Structure
1072959-67-1
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Field of application
SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1072959-67-1
Chemical Name: N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl-2,3-dihydro-1,4-benzodioxin-2-carboxamidedihydrochloride
Synonyms: SR-3677; SR 3677
SMILES: CN(C)CCOC1=C(NC(C2OC(C=CC=C3)=C3OC2)=O)C=CC(C4=CNN=C4)=C1
Formula: C22H24N4O4
M.Wt: 408.45
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
In Vivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing ex vivoaqueous 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[1].
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 nonkinase enzymes and receptors. The IC50 value of SR-3677 for ROCK-I is 56±12 nM. The hydrophobic interaction of the benzodioxane phenyl ring with the hydrophobic surface of the pocket is the dominating factor that contributes to the high potency of SR-3677[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC6902 Thiazovivin Thiazovivin is a rock inhibitor and enhances fibroblast reprogramming efficiency to generate stem cells
DC7246 SR3677 SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
DC8329 SLx-2119(KD-025,Belumosudil ) SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM)
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DC7269 RKI-1447 RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
DC8831 RKI-1313 RKI-1313 is the negative control for RKI-1447 which is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer
DC7774 Ripasudil(K-115) K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
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