| Field | Specification |
|---|---|
| Alternative names | HIF-1α inhibitor; LW8 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H29NO5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LW6, also known as HIF-1α inhibitor or LW8, is a novel HIF-1 inhibitor with an IC50 value of 4.4 μM, and it also inhibits MDH2. It decreases HIF-1α protein expression without affecting HIF-1β expression. It is supplied as a white to off-white solid (C26H29NO5, MW 435.51) at 98.86% purity.
Physical & Chemical Properties
| CAS Number | 934593-90-5 |
|---|---|
| Molecular Formula | C26H29NO5 |
| Molecular Weight | 435.51 g/mol |
| Purity | 98.86% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(OC)C1=CC=C(O)C(NC(COC2=CC=C(C3(C4)CC5CC4CC(C5)C3)C=C2)=O)=C1 |
| Signaling Pathway | Metabolic Enzyme/Protease; Apoptosis |
| Solubility | In Vitro: DMSO: 25 mg/mL (57.40 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) DMF: 17.24 mg/mL (39.59 mM; Requires sonication) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 4.4 μM (HIF-1)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (57.40 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| DMF | 17.24 mg/mL (39.59 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 2.5 mg/mL (5.74 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.74 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
The stability of the HIF-1α protein is affected by LW6 (0-20 μM; 12-16 h). LW6 promotes degradation of wild type HIF-1α but not of DM-HIF-1α, which carries P402A and P564A modifications at hydroxylation sites in the oxygen-dependent degradation domain. LW6 induces expression of von Hippel-Lindau (VHL), which binds prolyl-hydroxylated HIF-1α for proteasomal degradation. With LW6 present, VHL knockdown does not abolish HIF-1α protein accumulation, indicating that LW6 degraded HIF-1α by regulating VHL expression[2]. In MDCKII-BCRP cells overexpressing BCRP, LW6 (0.01-25 μM; 0-48 h) significantly enhances cellular accumulation of mitoxantrone, a BCRP substrate. LW6 also down-regulates BCRP expression at 0.1-10 μM[3]. In A549 cells, LW6 (5-100 μM; 12-48 h) inhibits hypoxia-induced HIF 1α expression at 20 μM, with no dependence on the von Hippel Lindau protein. Hypoxia-selective apoptosis is induced by LW6 together with a reduction in mitochondrial membrane potential[4].
In Vivo
In mice bearing xenografts of human colon cancer HCT116 cells, LW6 (intraperitoneal injection; 10-20 mg/kg; 13 days) shows strong anti-tumor efficacy in vivo and lowers HIF-1α expression, as seen by immunohistochemical staining of frozen tissue[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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