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ROCK inhibitor GSK269962A

  Cat. No.:  DC7249   Featured
Chemical Structure
850664-21-0
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More than 5000 active chemicals with high quality for research!
Field of application
GSK269962A(GSK269962) is a potent ROCK inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively); displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 850664-21-0
Chemical Name: N-[3-[[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]-benzamide
Synonyms: GSK269962; GSK 269962; GSK-269962; GSK269962A; GSK 269962A; GSK-269962A; GSK269962B.
SMILES: CCN1C2=CC(OC3=CC=CC(NC(C4=CC=C(OCCN5CCOCC5)C=C4)=O)=C3)=NC=C2N=C1C6=NON=C6N
Formula: C29H30N8O5
M.Wt: 570.61
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK269962A is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively.
In Vivo: Oral administration of GSK269965A (0.3, 1, and 3 mg/kg) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial. The maximal effect on blood pressure is observed approximately 2 h after oral gavages for both compounds. Under a similar setting, oral administration of Y-27632 (10 and 30 mg/kg) also induced a dose-dependent decrease of blood pressure. For all three Rho kinase inhibitors, the reduction of blood pressure is accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism[1].
In Vitro: GSK269962A IC50 values of 1.6 nM toward recombinant human ROCK1. GSK269962A also exhibits more than 30-fold selectivity against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM. Both are highly potent toward human ROCK1 with IC50 of 1.6 nM for GSK269962A. On the other hand, GSK269962A has a significantly improved kinase selectivity profile with at least >30-fold selectivity against the panel of protein kinase tested[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1028 Y-27632 2HCL Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM.
DC6902 Thiazovivin Thiazovivin is a rock inhibitor and enhances fibroblast reprogramming efficiency to generate stem cells
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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)
DC9854 SAR407899 SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
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.
DC9614 Hydroxyfasudil (hydrochloride) Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
DC7144 GSK429286A GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
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