GKT137831 supplier|GKT-137831|DC Chemicals

GKT137831 supplier|GKT-137831|DC Chemicals
DC Chemicals provides GKT137831, other names: GKT-137831,GKT 137831, cas: 784210-88-4. In stock.

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GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

GKT137831, other names: GKT-137831,GKT 137831, cas: 784210-88-4, Molecule formular: C29H35N7O4, Molecule Weight: 545.63, Chemical name: N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.RGB-286638 inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. RGB-286638 demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manifesting less cytotoxicity in healthy donor PBMCs. Treatment with RGB-286638 resulted in rapid downregulation of p-RNAPII S2/S5 across all tested MM cell lines. RGB-286638 (50nM) reduced the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but had no effects on p-Rb S780.
For the detailed information of GKT137831, the solubility of GKT137831 in water, the solubility of GKT137831 in DMSO, the solubility of GKT137831 in PBS buffer, the animal experiment (test) of  GKT137831, the cell expriment (test) of GKT137831, the in vivo, in vitro and clinical trial test of GKT137831, the EC50, IC50,and affinity,of GKT137831, Please contact DC Chemicals.