1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
    Autophagy
  2. ROCK
    Autophagy
  3. SR-3677

SR-3677 

Cat. No.: HY-13300 Purity: 99.46%
Handling Instructions

SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.

For research use only. We do not sell to patients.

SR-3677 Chemical Structure

SR-3677 Chemical Structure

CAS No. : 1072959-67-1

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10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
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100 mg USD 660 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.

IC50 & Target

ROCK-II

3 nM (IC50)

ROCK-I

56 nM (IC50)

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].

In Vivo

ExVivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing 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[1].

Molecular Weight

408.45

Formula

C₂₂H₂₄N₄O₄

CAS No.

1072959-67-1

SMILES

CN(C)CCOC1=C(NC(C2OC(C=CC=C3)=C3OC2)=O)C=CC(C4=CNN=C4)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 43 mg/mL (105.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4483 mL 12.2414 mL 24.4828 mL
5 mM 0.4897 mL 2.4483 mL 4.8966 mL
10 mM 0.2448 mL 1.2241 mL 2.4483 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Assays are performed using the STK2 kinase system from Cisbio. 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. 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 addition of 10 μL of 1x antibody and 62.5 nM Sa-XL in detection buffer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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