Home Angiogenesis HIF inhibitor CAY10585 (LW 6) For research use only.

CAY10585 (LW 6)

Synonyms: AC1-001

CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. LW6 inhibits HIF and MDH2 expression with IC50 values of 4.4 and 6.3 μM, respectively.

CAY10585 (LW 6) Chemical Structure

CAY10585 (LW 6) Chemical Structure

CAS No. 934593-90-5

Purity & Quality Control

CAY10585 (LW 6) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
AGS Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50=0.7μM 17328532
Hep3B Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay, IC50=2.6μM 17328532
Hep3B Function assay 10 uM Suppression of hypoxia-induced VEGF mRNA expression in human Hep3B cells at 10 uM 17328532
Hep3B Function assay 10 uM Suppression of hypoxia-induced EPO mRNA expression in human Hep3B cells at 10 uM 17328532
HCT116 Function assay 16 hrs Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay, IC50=2.44μM 23153200
HeLa Function assay 12 hrs Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay, IC50=21μM 24900662
HeLa Function assay 30 uM 4 hrs Inhibition of hypoxia-induced HIF1alpha nuclear translocation in human HeLa cells at 30 uM after 4 hrs by immunofluorescence analysis 24900662
HeLa Function assay 30 uM 4 hrs Inhibition of hypoxia-induced HIF1alpha accumulation in human HeLa cells at 30 uM after 4 hrs by Western blot analysis 24900662
HCT116 Function assay 12 hrs Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay, IC50=4.4μM 25356789
HCT116 Function assay 10 uM Reduction in ATP production in human HCT116 cells at 10 uM by luciferase based assay 25356789
HCT116 Function assay 10 uM Inhibition of MDH2 in human HCT116 cells assessed as AMPK activation at 10 uM by immunoblot assay 25356789
HCT116 Function assay 10 uM Inhibition of MDH2 in human HCT116 cells assessed as reduction in ACC phosphorylation at 10 uM by immunoblot assay 25356789
HCCLM3 Function assay Inhibition of HIF1alpha transcriptional activity in hypoxia-induced human HCCLM3 cells co-transfected with luciferase reporter plasmid containing five copies of HREs and pRL-SV40 plasmid encoding Renilla luciferase incubated with compound under normoxia f, IC50=3.08μM 31556611
HCCLM3 Function assay 10 uM 1 hr Inhibition of HIF1alpha accumulation in hypoxia-induced human HCCLM3 cells at 10 uM incubated with compound under normoxia for 1 hr followed by hypoxia induction and measured after 24 hrs by Western blot analysis 31556611
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Biological Activity

Description CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. LW6 inhibits HIF and MDH2 expression with IC50 values of 4.4 and 6.3 μM, respectively.
Targets
BCRP [3] HIF [2]
(Cell-free assay)		 MDH2 [2]
(Cell-free assay)
4.4 μM 6.3 μM
In vitro
In vitro

LW6 inhibits HIF-1α expression induced by hypoxia. It promotes apoptosis preferentially in hypoxic cells. Treatment with LW6 presents no additive effect on cell cycle arrest. LW6 induces ROS formation through the depolarization of MMP in hypoxic cells. Although LW6 increases mitochondrial ROS production, the combination with hypoxia induces a marked increase in ROS production and this high level is maintained up until 24 h. LW6 is also a specific inhibitor of MDH2. As MDH2 is known to serve a significant role in the citric acid cycle at the mitochondrial membrane, LW6 indirectly reduces the activity of the mitochondrial respiratory chain through the inhibition of MDH2[1].In contrast to BCRP, LW6 has no inhibition effect on the functional activity and gene expression of P-gp[2]. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM. Furthermore, cells become more susceptible to the cytotoxicity of anticancer drugs in the presence of LW6[3].
Cell Research Cell lines A549 cells
Concentrations 5-100 μM
Incubation Time 24 h
Method

Cells are incubated in 96-well ELISA Plates with 100 μl culture medium at 2×105 cells/ml with or without LW6 for 24 h. Cell viability is assessed by the dimethyl thiazolcarboxy-methoxyphenylsulfophenyltetrazolium (MTS) assay. The absorbance is measured at 490 and 620 nm using a microplate reader. For the trypan blue dye. exclusion test, cells are stained by phosphate-buffered saline (PBS) containing 0.1% trypan blue. Cell viability is assessed by counting the number of unstained cells.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-1α E-cadherin / PIMT 26017562
In Vivo
In vivo

LW6 exerts marked anti-tumor efficacy in vivo and causes reductions in HIF-1α expression levels in mice carrying xeno-grafts of HCT116 cells[1]. LW6 improves the cytotoxicity and bioavailability of anticancer drugs translocated by BCRP[3].
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 10 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 435.51 Formula

C26H29NO5
CAS No. 934593-90-5 SDF Download CAY10585 (LW 6) SDF
Smiles COC(=O)C1=CC(=C(C=C1)O)NC(=O)COC2=CC=C(C=C2)C34CC5CC(C3)CC(C5)C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 24 mg/mL ( (55.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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