Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-[1,1-dimethyl-2-(4-methyl-1-piperazinyl)-2-oxoethyl]-N-[6-(4-pyridinyl)imidazo[1,2-a]pyridin-2-yl]-benzamide
Purity: ≥98%
Formula Markup: C28H30N6O2
Formula Weight: 482.6
CAS Number: 2109805-56-1
Notes: T3-CLK is a pan inhibitor of CDC-like kinases (Clks; IC50s = 0.67, 15, and 110 nM for Clk1, Clk2, and Clk3, respectively).{68854} It is selective for Clk1-3 over dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) and DYRK1B (IC50s = 260 and 230 nM, respectively), as well as 62 kinases in a panel at 1,000 nM and four kinases in the same panel at 1,110 nM. T3-CLK modulates Clk-responsive alternative splicing events and reduces exon recognition, as well as increases levels of conjoined gene transcripts, in HCT116 colorectal cancer cells and 184-hTERT mammary epithelial cells. It reduces the expression of VEGFR2 in human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 300 to 1,000 nM.{68855} T3-CLK also inhibits VEGF-induced-sprouting in HUVEC spheroids when used at concentrations of 300 and 1,000 nM and inhibits HUVEC migration at 500, 800, and 1,000 nM.
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