Table 1. The Targets and Mechanisms of HIF Inhibitors for Cancer Therapy.
| Agents | Inhibitory mechanisms | CAS no. | Targeting HIF-1 | Targeting HIF-2 | References no. |
|---|---|---|---|---|---|
| EZN-2968* | HIF-1 mRNA expression | Yes | No | 30, 31 | |
| EZN-2208† | HIF-1 mRNA expression | Yes | NS | 32 | |
| Topotecan | HIF-1 mRNA translation | 123948-87-8 | Yes | NS | 33 |
| PX-478 | HIF-1α mRNA expression and translation | 685898-44-6 | Yes | NS | 34 |
| 2-methoxyestradiol | HIFα protein synthesis, nuclear translocation and transcriptional activity | 362-07-2 | Yes | Yes | 35, 36 |
| KC7F2 | HIF-1α protein synthesis | 927822-86-4 | Yes | NS | 37 |
| Glyceollins | HIF-1α protein synthesis and stability | Yes | NS | 38 | |
| CAY10585 | HIF-1 protein synthesis and transcriptional activity | 934593-90-5 | Yes | No | 39 |
| 17-AAG | Promoting HIFα degradation | 75747-14-7 | Yes | Yes | 40 |
| 17-DMAG | Promoting HIFα degradation | 467214-21-7 | Yes | Yes | 41 |
| Bisphenol A | Promoting HIF-1α degradation | 1568-83-8 | Yes | NS | 42 |
| BAY 87-2243 | HIFα protein accumulation | 1227158-85-1 | Yes | Yes | 43 |
| Cryptotanshinone | HIF-1α protein accumulation | 35825-57-1 | Yes | NS | 44 |
| Vorinostat | Promoting HIFα degradation | 149647-78-9 | Yes | Yes | 45 |
| LW6 | HIF-1α protein stability | 934593-90-5 | Yes | NS | 46 |
| HIF-1α inhibitor | HIFα protein accumulation and transcriptional activity | 934593-90-5 | Yes | Yes | 47 |
| PX-12 | HIFα protein accumulation and transcriptional activity | 141400-58-0 | Yes | NS | 48, 49 |
| TAT-cyclo-CLLFVY‡ | Selective HIF-1 dimerization inhibitor | 1446322-66-2 | Yes | No | 50 |
| TC-S7009 | HIF-2 heterodimerization and DNA binding | 1422955-31-4 | No | Yes | 51 |
| PT2385 | HIF-2 heterodimerization and DNA binding | 1672665-49-4 | No | Yes | 52 |
| Acriflavine | HIF dimerization and transcriptional activity | 8048-52-0 | Yes | Yes | 53 |
| Echinomycin | HIF DNA binding | 512-64-1 | Yes | NS | 54, 55 |
| Indenopyrazole 21 | HIF-1 transcriptional activity | 1421448-26-1 | Yes | NS | 65 |
| FM19G11 | HIF transcriptional activity | 329932-55-0 | Yes | Yes | 55, 67 |
| YC-1 | HIFα protein accumulation and transcriptional activity | 170632-47-0 | Yes | Yes | 66 |
| NSC 607097 | HIF-1 transcriptional activity and protein accumulation | 497181-30-3 | Yes | No | 70 |
HIF, hypoxia-inducible factor; NS, not studied.
*An antisense oligodeoxynucleotide agent, †A water-soluble, polyethylene glycol drug conjugate of SN38, the active moiety of irinotecan, ‡A peptide agent.