Aurora Kinase Ligand
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Quercimeritrin
0 ImagesQuercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer.
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SF-1
0 ImagesCat. No.: HY-168545Purity: 99.50%SF-1 is an AURKA ligand that can be used for the synthesis of PROTACs, such as PROTAC MPS1 degrader 2 (HY-168543). SF-1 can act as a free inhibitor and has the ability to pull down AURKA, AURKB, and TTK with DC50 values of 273.5, 933.5, and 1274 nM respectively. SF-1 has an anti-proliferative effect on acute myeloid leukemia.
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HLDA-212
0 ImagesCat. No.: HY-173499CAS No.: 3077339-88-6HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies).
