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. 2023 Jul 22;13(11):4341–4372. doi: 10.1016/j.apsb.2023.07.019

Table 1.

List of representative anticancer small molecules by targeting E2s, CRLs or DUBs.

Name Structure Target In vitro In cells Cell viability, IC50 Cancer cell lines Ref.
CC0651 Image 1 Cdc34 IC50 (FP) = 2.5 μmol/L p27 deubiquitination @ 30 μmol/L HCT116 280,281
Leucettamol A Image 2 Ubc13 105 μmol/L 282
2D-08 Image 3 Ubc9 IC50 = 6 μmol/L 100 μmol/L BT-474 283
Compound 25 Image 4 CRL1Skp2 >80% inhibition@5 μmol/L p21, p27 deubiquitination @ 5 μmol/L <10 μmol/L PC-3, LNCaP 293
C1, C2, C16, C20 Image 5 >80% inhibition@10 μmol/L p21, p27 deubiquitination @ 10 μmol/L MCF-7, TD47, LNCaP 294
VH298 Image 6 CRL2VHL IC50 (FP) = 80 nmol/L;
Kd (ITC) = 90 nmol/L		 HIF-1α destabilization @ 50 μmol/L No cytotoxic Hela 299
CM11 homo-PROTAC Kd (ITC) = 25 nmol/L HIF-1α destabilization @ 1 μmol/L Hela 300
CDDO-Me Image 7 CRL3Keap1 58.9%@0.1 μmol/L 50–160 nmol/L MCF-7 302
ML334 Image 8 Kd = ∼ 1 μmol/L EC50 = 18 μmol/L U2OS 303
Compound 2 Image 9 EC50 = 28.6 nmol/L Nrf2–ARE induction@10 μmol/L HepG2-ARE-C8 304
KI696 Image 10 Kd (ITC) = 1.3 nmol/L 305
6lc Image 11 CRL3SPOP KD = 30 μmol/L PTEN deubiquitination @ 15 μmol/L 2.1–3.5 μmol/L A498, OS-RC-2 308,309
CC885 Image 12 CRL4CRBN GSPT1 degradation @ 1 nmol/L NB4 189
Thalidomid Image 13 336
Pomalidomide Image 14 337
Lenalidomid Image 15 IKZF1 and IKZF3 degradation @ 1 μmol/L MM1S 191,338
Indisulam Image 16 CRL4DCAF15 RBM39 degradation @ 2 μmol/L HCT116 339
CR8 Image 17 Cyclin K degradation @ 1 μmol/L HCT116 340
HQ461 Image 18 DC50 = 0.13 μmol/L 1.5 μmol/L A549 341
dCeMM2/3/4 Image 19 Cyclin K degradation @ 2.5 μmol/L KBM7 342
SJB2-043 Image 20 USP1 0.54 μmol/L >80% inhibition @ 1 μmol/L 1.1 μmol/L K562 347
ML323 Image 21 76 nmol/L PCNA deubiquitination @ 20 μmol/L 3 μmol/L H1299 348
Q29 Image 22 USP2 82% inhibition @ 0.5 μmol/L NA 4.7 μmol/L DU145 350
ML364 Image 23 1.1–1.7 μmol/L cyclin D1 destabilization @ 0.97 μmol/L 3 μmol/L HCT116 351
LCAHA Image 24 9.7 μmol/L cyclin D1 destabilization @ 20 μmol/L 0.9 μmol/L HCT116 352
XL188 Image 25 USP7 90 nmol/L p53 accumulation @5 μmol/L MM.1S, MCF7 357
FT671 Image 26 52 nmol/L p53 accumulation @10 μmol/L 33 nmol/L HCT116, MM.1S, MCF7 358
Compound 4 Image 27 6 nmol/L p53 accumulation @1 μmol/L 2–29 nmol/L HCT116 359
Compound 41 Image 28 0.44 nmol/L p53 accumulation @25 nmol/L 0.09–0.45 μmol/L MM.1S, H526 360
GNE6640 Image 29 0.75 μmol/L p53 accumulation @10 μmol/L >50% inhibition@5 μmol/L HCT116, MCF7, EOL-1 361
Capzimin Image 30 Rpn11 0.39 μmol/L Deubiquitination @ 2–10 μmol/L 2.1–3.8 μmol/L 293T, A549, HCT116 364
SOP11 Image 31 1.3/0.6 μmol/L Deubiquitination @ 10 μmol/L GI50 = 4.7 μmol/L HCT116 365
VLX1570 Image 32 USP14/UCH37 8.1/14 μmol/L >80% inhibition @ 25 mmol/L 43–126 nmol/L RPMI8226, KMS11, OPM-2 366