Skip to main content

View full-text article in PMC

. Author manuscript; available in PMC: 2022 Feb 16.

Published in final edited form as: J Med Chem. 2019 Dec 10;62(24):11280–11300. doi: 10.1021/acs.jmedchem.9b01530

Table 6.

Degradation Potencies of STAT3 Protein and Cell Growth-Inhibitory Activities of STAT3 Degraders in the Molm-16 and SU-DHL-1 Cell Lines

	Molm-16		SU-DHL-1
compd	DC₅₀ (STAT3, μM), 4 h	IC₅₀ ± SD (μM), 4 days	DC₅₀ (STAT3, μM), 16 h	IC₅₀ ± SD (μM), 4 days
SI-109 (8)	>10	6.45 ± 4.16	>10	>10
12	2.63	0.95 ± 0.081	nt^a	nt^a
13	0.26	0.078 ± 0.029	nt^a	nt^a
SD-36 (14)	0.06	0.013 ± 0.010	0.028	0.61 ± 0.014
15	0.09	0.025 ± 0.007	nt^a	nt^a
16	0.15	0.042 ± 0.004	nt^a	nt^a
17	0.65	0.147 ± 0.027	0.919	>10
18	0.24	0.128 ± 0.050	0.049	2.37 ± 0.70
19	0.05	0.091 ± 0.081	0.011	0.43 ± 0.16
20	0.18	0.241 ± 0.246	nt^a	nt^a
21	0.25	0.232 ± 0.175	nt^a	nt^a
22	0.18	0.099 ± 0.054	nt^a	nt^a
23	2.47	0.36 ± 0.056	nt^a	nt^a
24	0.38	0.067 ± 0.032	nt^a	nt^a
25	0.16	0.063 ± 0.016	nt^a	nt^a
26	0.09	0.059 ± 0.016	nt^a	nt^a
27	3.54	0.582 ± 0.654	>10	>10
28	0.41	0.104 ± 0.071	nt^a	nt^a
29	0.36	0.711 ± 0.262	nt^a	nt^a
30	0.22	0.210 ± 0.109	0.055	3.24 ± 0.57
31	0.64	0.226 ± 0.114	0.89	>10
32	>10	>2	nt^a	nt^a
33	>10	>2	nt^a	nt^a
34	4.45	1.25 ± 0.71	>10	>10
SD-36Me (35)	>10	5.21 ± 6.04	>10	>10

^a

Not tested.