Chemical Structure : AK-1690
Catalog No.: PC-23176Not For Human Use, Lab Use Only.
AK-1690 is the first, potent and selective PROTAC STAT6 degrader with DC50 of 1 nM in MV4;11 cells, Dmax>95%.
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AK-1690 is the first, potent and selective PROTAC STAT6 degrader with DC50 of 1 nM in MV4;11 cells, Dmax>95%.
AK-1690 shows no significant effect on STAT1, STAT3, STAT5, and pSTAT5Y694 up to 10 μM, and modest effect on STAT2 protein at 2 and 10 μM, with a maximum reduction of STAT2 protein of <40%.
AK-1690 effectively depleted STAT6 with a DC50 value of 80 nM and a Dmax value of >90% in in human peripheral blood mononuclear cells (PBMCs).
AK-1690 effectively induces depletion of phosphorylated STAT6 (pSTAT6Y641).
AK-1690 is a potent and selective STAT6 degrader over other STAT members and >6,000 other proteins.
AK-1690 has no effect on cereblon neo-substrates IKZF1 and IKZF3, as well as IKZF2 and GSPT1, in the Jurkat cell line.
AK-1690 (200 mg/kg, i.p.) effectively depleted STAT6 protein in mouse lung and liver tissues.
M.Wt | 1016.06 | |
Formula | C51H56F2N5O11PS | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Kaneshige A, et al. J Med Chem. 2024 Sep 23. doi: 10.1021/acs.jmedchem.4c01009.
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