Table 1.

Compounds reported to inhibit HIF-1α

CompoundHIF-1α Levels IC50m)HIF-1 Activity IC50m)Cytotoxicity IC50m)Mechanism of HIF-1α InhibitionIn Vivo HIF-1 LevelsRef.
Hsp-90 inhibitor
    Radicicol1.01.41.4DNA binding(39)
    KF58333 (radicicol analogue)0.1–0.50.1not decrease(40)
    Geldanamycin5.0breakdown(6)
10.00.05breakdown(41)
Flavonoid
    Genestein100(56)
150150(57)
Topoisomerase inhibitor
    Topotecan (topo-I)0.100.050.04–1.0translation(44, 45)
    GL331 (topo-II)10.00.2–2.0transcription(46)
Antimicrotubule
    Taxol0.01–0.10.001translation(42)
    Vincristine0.01–0.1(42)
    2-Methoxyestradiol1.0–5.01001.0translation(42)
Histone deacetylase inhibitor
    FK2282–20 nm0.3 nmtranscriptionnot decrease(47)
PI-3-kinase pathway inhibitor
    LY29400210.0–50.010–20(48)
40(58)
    Wortmannin0.01–0.105.0–20.0(48)
    Rapamycin0.01–0.050.005translation(8, 48)
MEK1 Inhibitor
    PD98059100>10(58)
100100transactivation(57)
Soluble guanyl cyclase stimulator
    YC-15.0–10.05.0–50.0transcriptiondecrease(53)
Thioredoxin inhibitor
    PX-127.211.52.0–3.0decrease(54)
    Pleurotin7.69.01.0decrease(54)
Other
    UCNO-1 (ser/thre kinase inhibitor)0.10.2–1.0kinase inhibition(59)
    Diphenylene iodonium1.0redox inhibition(60)
    Carboxyamido-triazole (Ca2+ blocker)1.0–5.05.0transcription(61)
    PX-4785.0–25.05.0–25.05.0–25.0breakdowndecrease(55)