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LW6

Cat. No. M9279

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LW6 Structure
Synonym:

HIF-1α inhibitor; CAY10585

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 63  USD63 In stock
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
25mg USD 190  USD190 In stock
50mg USD 319  USD319 In stock
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Quality Control & Documentation
Biological Activity

LW6 is a novel HIF-1alpha inhibitor, with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.

LW6 decreased HIF-1alpha protein expression without affecting HIF-1beta expression. LW6 promoted the degradation of wild type HIF-1alpha, but not of a DM-HIF-1alpha with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain (ODDD). LW6 did not affect the activity of prolyl hydroxylase (PHD), but induced the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1alpha for proteasomal degradation.

In mice carrying xenografts of human colon cancer HCT116 cells, LW6 demonstrated strong anti-tumor efficacy in vivo and caused a decrease in HIF-1alpha expression in frozen-tissue immunohistochemical staining.

Chemical Information
Molecular Weight 435.51
Formula C26H29NO5
CAS Number 934593-90-5
Solubility (25°C) DMSO 25 mg/mL
DMF 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Song JG, et al. Cancer Chemother Pharmacol. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein.

[2] Sato M, et al. Mol Med Rep. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells.

[3] Lee K, et al. Biochem Pharmacol. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line.

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Abmole Inhibitor Catalog




Keywords: LW6, HIF-1α inhibitor; CAY10585 supplier, HIF, inhibitors, activators

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