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WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively. WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. Treatment of MEFs with WM-1119 results in cell cycle arrest in G1 and a senescence phenotype. WM-1119 arrests the progression of lymphoma in mice. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).
Molecular Weight | 389.38 |
Formula | C18H13F2N3O3S |
CAS Number | 2055397-28-7 |
Solubility (25°C) | DMSO 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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