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Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. Also reduces tubularization of hypoxic HUVECs.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $1,180 | 35 days | 35 days |
| Description | Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. Also reduces tubularization of hypoxic HUVECs. |
| Molecular Weight | 2559.1 |
| Formula | C111H188N42O24S2 |
| Cas No. | 1446322-66-2 |
| Smiles | C(=O)([C@H]1N(C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@H](CSSC[C@@H]2NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H]([C@@H](C)C)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC2=O)N)=O)=O)CCCNC(=N)N)=O)CCCCN)=O)CCCCN)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCC(N)=O)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCC1)N5[C@H](C(N[C@@H](CCC(N)=O)C(O)=O)=O)CCC5 |
| Relative Density. | 1.51 g/cm3 (Predicted) |
| Sequence | H-Cys(1)-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Gln-OH.cyclo[Cys(1)-Leu-Leu-Phe-Val-Tyr] |
| Sequence Short | CGRKKRRQRRRPPQ |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O: 1 mg/mL (0.39 mM), Sonication is recommended. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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