T3-CLK

T3-CLK is a pan inhibitor of CDC-like kinases (Clks, IC50s = 0.67, 15, and 110 nM for Clk1, Clk2, and Clk3, respectively). 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. 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.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. CAS Number: 2109805-56-1. Synonyms: CDC-like Kinase Inhibitor T3, CDC-like Kinase-IN-T3, CLK-IN-T3, T3-CDC-like Kinase. Molecular Formula: C28H30N6O2. Formula Weight: 482.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: O=C(C1=CC=C(C(C)(C)C(N2CCN(CC2)C)=O)C=C1)NC3=CN4C=C(C5=CC=NC=C5)C=CC4=N3. InChi Code: InChI=1S/C28H30N6O2/c1-28(2,27(36)33-16-14-32(3)15-17-33)23-7-4-21(5-8-23)26(35)31-24-19-34-18-22(6-9-25(34)30-24)20-10-12-29-13-11-20/h4-13,18-19H,14-17H2,1-3H3,(H,31,35). InChi Key: IEFFSHLHNYVSEF-UHFFFAOYSA-N.