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LW6

Catalog No. T3494 CAS 934593-90-5

Synonyms: HIF-1α inhibitor, CAY10585, LW8

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.

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LW6, CAS 934593-90-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 91.00
25 mg	In stock	$ 193.00
50 mg	In stock	$ 313.00
100 mg	In stock	$ 472.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.10%

Purity: 98.1%

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Description	LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.
Targets&IC50	MDH2:6.3 μM, HIF:4.4 μM
In vitro	LW6 decreases the expression of HIF-1α protein without affecting HIF-1β expression. LW6 affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α while not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain. LW6 induces the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation. The knockdown of VHL does not abolish HIF-1α protein accumulation in the presence of LW6 which indicates that LW6 degraded HIF-1α via regulation of VHL expression[2]. In MDCKII-BCRP cells overexpressing BCRP, LW6 enhances significantly the cellular accumulation of mitoxantrone, a BCRP substrate. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM[3]. LW6 inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 mM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential[4].
In vivo	LW6 exhibits potent anti-tumor activity in vivo, leading to reduced HIF-1α expression as observed through immunohistochemical staining of frozen tissues in mice with xenografts derived from human colon cancer HCT116 cells[2].
Cell Research	Inhibition of HIF-1a is assayed by a reporter assay using dualluciferase reporter assay system. HCT116 cells in 75-90% confluence are transiently co-transfected with pGL3-HRE-luciferase plasmid containing six copies of HREs from human VEGF genes and pRLSV40 encoding firefly renilla luciferase and incubated for 24 h. Cells are treated with LW6 or 17-AAG for 16 h before report assay. Luciferase activity is integrated over a 10 second period and measured using a luminometer[2].

Synonyms	HIF-1α inhibitor, CAY10585, LW8
Molecular Weight	435.51
Formula	C26H29NO5
CAS No.	934593-90-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (114.81 mM)

References and Literature

1. Naik R , Won M , Ban H S , et al. Synthesis and Structure–Activity Relationship Study of Chemical Probes as Hypoxia Induced Factor-1α/Malate Dehydrogenase 2 Inhibitors[J]. Journal of Medicinal Chemistry, 2014, 57(22):9522-9538. 2. Lee K, et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9. 3. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein. 4. Sato M, et al. LW6, a hypoxia-inducible factor 1 inhibitor, selectively induces apoptosis in hypoxic cells through depolarization of mitochondria in A549 human lung cancer cells. Mol Med Rep. 2015 Sep;12(3):3462-8. 5. Zhu B, Wu Y, Huang S, et al. Uncoupling of macrophage inflammation from self-renewal modulates host recovery from respiratory viral infection[J]. Immunity. 2021

Citations

1. Zhu B, Wu Y, Huang S, et al. Uncoupling of macrophage inflammation from self-renewal modulates host recovery from respiratory viral infection. Immunity. 2021, 54(6): 1200-1218. e9.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Epigenetics Compound Library Bioactive Compounds Library Max Glycometabolism Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library Bioactive Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

LW6 934593-90-5 Angiogenesis Apoptosis Chromatin/Epigenetic Metabolism Dehydrogenase HIF/HIF Prolyl-Hydroxylase HIF LW 6 HIF-1α inhibitor Hypoxia-inducible factors inhibit CAY10585 HIF-PH CAY-10585 LW-6 HIFs LW 8 Inhibitor LW-8 HIF-1alpha inhibitor LW8 HIF-1a inhibitor CAY 10585 inhibitor

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