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LW6

Cat. No. M9279
LW6 Structure
Synonym:

HIF-1α inhibitor; CAY10585

Size Price Availability Quantity
10mM*1mL In DMSO USD 79 In stock
5mg USD 72 In stock
10mg USD 108 In stock
25mg USD 236 In stock
50mg USD 420 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 435.51
Formula C26H29NO5
CAS Number 934593-90-5
Purity 99.42%
Solubility DMSO: ≥ 20 mg/mL
Storage at -20°C
References

Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein.
Song JG, et al. Cancer Chemother Pharmacol. 2016 Oct;78(4):735-44. PMID: 27520631.

LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells.
Sato M, et al. Mol Med Rep. 2015 Sep;12(3):3462-3468. PMID: 26017562.

LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line.
Lee K, et al. Biochem Pharmacol. 2010 Oct 1;80(7):982-9. PMID: 20599784.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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