LW6
Based on 63 publication(s) in Google Scholar
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
For research use only. We do not sell to patients.
- Purity: 98.86%
- CAS No.: 934593-90-5
- Formula: C26H29NO5
- Molecular Weight:435.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Reprogramming Compound Library
HY-L039
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Oxygen Sensing Compound Library
HY-L045
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Cancer Metabolism Compound Library
HY-L083
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Angiogenesis-Related Compound Library
HY-L088
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Transcription Factor-Targeted Library
HY-L090
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Targeted Diversity Library
HY-L099
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Anti-Prostate Cancer Compound Library
HY-L124
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Cancer Stem Cells Compound Library
HY-L135
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Metabolic Enzyme Compound Library
HY-L146
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Cell Death Library
HY-L162
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Fibrosis Compound Library
HY-L185
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Lactic Acid Metabolic Compound Library
HY-L204
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) LW6
More- Cell Metab. 2023 Aug 8;35(8):1390-1405.e8. [Abstract]
- Autophagy. 2025 Aug;21(8):1824-1842. [Abstract]
- Acta Pharm Sin B. 2025 Mar;15(3):1514-1534. [Abstract]
- Adv Sci (Weinh). 2025 May 20:e17128. [Abstract]
- Adv Sci (Weinh). 2025 Apr 28:e2409837. [Abstract]
- Adv Sci (Weinh). 2025 Mar 24:e2411980. [Abstract]
- Adv Sci (Weinh). 2024 Dec 5:e2410360. [Abstract]
- Adv Sci (Weinh). 2024 Dec 25:e2407134. [Abstract]
- Adv Sci (Weinh). 2024 Jul 15:e2404119. [Abstract]
- Cell Rep Med. 2026 Feb 17;7(2):102616. [Abstract]
- Cell Death Dis. 2021 May 14;12(5):490. [Abstract]
- Phytomedicine. 2024 Jul:129:155647. [Abstract]
- J Hazard Mater. 2024 Sep 23:480:135937. [Abstract]
- Acta Pharmacol Sin. 2025 Jul;46(7):1974-1989. [Abstract]
- J Transl Med. 2024 Dec 20;22(1):1135. [Abstract]
- Dev Cell. 2026 Apr 29:S1534-5807(26)00150-4. [Abstract]
- Chin Med J (Engl). 2025 Sep 17. [Abstract]
- Oncogene. 2023 Jan;42(3):184-197. [Abstract]
- Antioxidants (Basel). 2024 Jul 14;13(7):840. [Abstract]
- Stem Cell Res Ther. 2025 Feb 4;16(1):40. [Abstract]
- Aging Cell. 2024 Dec;23(12):e14332. [Abstract]
- Chin Med. 2024 Mar 1;19(1):37. [Abstract]
- Redox Rep. 2025 Dec;30(1):2544412. [Abstract]
- J Ethnopharmacol. 2025 May 29:119943. [Abstract]
- J Agric Food Chem. 2025 Oct 22;73(42):26621-26632. [Abstract]
- Biomater Adv. 2025 May 27:176:214342. [Abstract]
- Ocul Surf. 2026 Jan 21:40:12-21. [Abstract]
- Ecotoxicol Environ Saf. 2024 May 22:279:116481. [Abstract]
- Biochem Pharmacol. 2024 May 14:225:116294. [Abstract]
- Life Sci. 2026 Mar 15:389:124253. [Abstract]
- Food Funct. 2025 Jan 20;16(2):628-639. [Abstract]
- Eur J Pharmacol. 2023 Sep 5:954:175858. [Abstract]
- Eur J Pharmacol. 2023 Jun 15:949:175725. [Abstract]
- Eur J Pharmacol. 2022 Sep 5:930:175154. [Abstract]
- Int Immunopharmacol. 2026 Jun 1:178:116522. [Abstract]
- Biomolecules. 2025 Feb 10;15(2):256. [Abstract]
- Int J Mol Sci. 2023 Jun 16;24(12):10236. [Abstract]
- J Cyst Fibros. 2025 Aug 15:S1569-1993(25)01561-9. [Abstract]
- Invest Ophthalmol Vis Sci. 2025 Jun 2;66(6):32. [Abstract]
- Arthritis Res Ther. 2025 Sep 26;27(1):180. [Abstract]
- Front Cell Dev Biol. 2021 Sep 1;9:718707. [Abstract]
- Chem Biol Interact. 2026 Jan 5:423:111838. [Abstract]
- Mediators Inflamm. 2026;2026(1):e7440641. [Abstract]
- Transl Oncol. 2026 Jun 18:71:102847. [Abstract]
- Sci Rep. 2025 Nov 17;15(1):40227. [Abstract]
- Cell Signal. 2021 Nov:87:110140. [Abstract]
- J Neurochem. 2025 Jan;169(1):e16281. [Abstract]
- Biomedicines. 2026 May 18;14(5):1145. [Abstract]
- Biomedicines. 2024 Nov 20;12(11):2649. [Abstract]
- iScience. 2021 May 7;24(6):102521. [Abstract]
- Front Physiol. 2020 Jun 30;11:669. [Abstract]
- Vet Res. 2025 Apr 30;56(1):94. [Abstract]
- Exp Cell Res. 2025 Mar 15;446(2):114451. [Abstract]
- Exp Eye Res. 2025 Oct:259:110576. [Abstract]
- Genes (Basel). 2023 Apr 30;14(5):1024. [Abstract]
- Toxicol In Vitro. 2024 Feb:94:105724. [Abstract]
- Am J Drug Alcohol Abuse. 2025 May 27:1-11. [Abstract]
- J Chem Neuroanat. 2021 Oct:116:101994. [Abstract]
- Biochem Biophys Res Commun. 2022 Aug 30;617(Pt 2):55-61. [Abstract]
- J Appl Genet. 2020 Feb;61(1):105-112. [Abstract]
- bioRxiv. 2025 January 18.
- Research Square Preprint. 2024 Apr 5.
- Oxid Med Cell Longev. 2022 Jan 29:2022:4566851. [Abstract]
Customer Validation & Images
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RT-PCR
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WB
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Flow Cytometry
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Flow Cytometry
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WB
Biological Activity
IC50: 4.4 μM (HIF-1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
0.7 μM
Compound: 23
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Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay
Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay
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[PMID: 17328532] |
| HCCLM3 | CC50 |
>50 μM
Compound: 1; LW6
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Cytotoxicity against human HCCLM3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HCCLM3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 31556611] |
| HCT-116 | IC50 |
>30 μM
Compound: CAY10585
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Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| HCT-116 | IC50 |
2.44 μM
Compound: 1, LW6
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Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
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[PMID: 23153200] |
| HCT-116 | IC50 |
4.4 μM
Compound: LW6
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Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay
Inhibition of HIF-1alpha in human HCT116 cells incubated for 12 hrs under hypoxic conditions by Western blotting and HRE-luciferase reporter assay
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[PMID: 25356789] |
| HeLa | IC50 |
>30 μM
Compound: CAY10585
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| HeLa | IC50 |
21 μM
Compound: CAY10585
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Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
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[PMID: 24900662] |
| Hep 3B2 | IC50 |
2.6 μM
Compound: 23
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Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay
Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay
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[PMID: 17328532] |
| HepG2 | IC50 |
>30 μM
Compound: CAY10585
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Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| PC-3 | IC50 |
>30 μM
Compound: CAY10585
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Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
LW6 (0-20 μM; 12-16 h) affects the stability of the HIF-1α protein. LW6 promotes the degradation of wild type HIF-1α, but 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. In the presence of LW6, knockdown of VHL does not abolish HIF-1α protein accumulation, indicating that LW6 degraded HIF-1α via regulation of VHL expression[2].
LW6 (0.01-25 µM; 0-48 h) enhances significantly the cellular accumulation of mitoxantrone, a BCRP substrate in MDCKII-BCRP cells overexpressing BCRP. LW6 also down-regulates BCRP expression at concentrations of 0.1-10 μM[3].
LW6 (5-100 μM; 12-48 h) inhibits the expression of HIF 1α induced by hypoxia in A549 cells at 20 μM, independently of the von Hippel Lindau protein. LW6 induces hypoxia selective apoptosis together with a reduction in the mitochondrial membrane potential[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 934593-90-5
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Appearance Solid
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Molecular Weight 435.51
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Formula C26H29NO5
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Color White to off-white
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SMILES
O=C(OC)C1=CC=C(O)C(NC(COC2=CC=C(C3(C4)CC5CC4CC(C5)C3)C=C2)=O)=C1
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Synonyms
HIF-1α inhibitor; LW8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (63)
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Journal Impact Factor
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Most Recent
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Cell Metab
UBE2M-mediated neddylation of TRIM21 regulates obesity-induced inflammation and metabolic disorders. [Abstract]2023 Aug 8;35(8):1390-1405.e8. PMID: 37343564 -
Autophagy
H3K36me2 methyltransferase NSD2/WHSC1 promotes triple-negative breast cancer metastasis via activation of ULK1-dependent autophagy. [Abstract]2025 Aug;21(8):1824-1842. PMID: 40097917
LW6 purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Aug;21(8):1824-1842. [Abstract]
TNBC cells following LW6 treatment (10 μM) or vehicle were cultured under normoxia or hypoxia, and expression of NSD2 was detected using qRT-pcr.
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Acta Pharm Sin B
Dihydromyricetin mitigates abdominal aortic aneurysm via transcriptional and post-transcriptional regulation of heme oxygenase-1 in vascular smooth muscle cells. [Abstract]2025 Mar;15(3):1514-1534. PMID: 40370559
LW6 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Mar;15(3):1514-1534. [Abstract]
Western blot analysis showed that LW 6 (20 μmol/L) partially reversed DHM-induced HO-1 protein expression, although levels remained significantly higher than the control group.
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Adv Sci (Weinh)
Pyruvate Carboxylase in Macrophages Aggravates Atherosclerosis by Regulating Metabolism Reprogramming to Promote Inflammatory Responses Through the Hypoxia-Inducible Factor-1 Signaling Pathway. [Abstract]2025 May 20:e17128. PMID: 40391718 -
Adv Sci (Weinh)
Microbiota-Derived Inosine Suppresses Systemic Autoimmunity via Restriction of B Cell Differentiation and Migration. [Abstract]2025 Apr 28:e2409837. PMID: 40289872
LW6 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 28:e2409837. [Abstract]
Representative figures and statistical analysis of frequencies of ASC with or without LW6 (10 µm) in human peripheral blood B cells culture for 48 h.
LW6 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 28:e2409837. [Abstract]
Frequencies of ASC with or without LW6 (10 µm) or inosine in mouse splenic B cells cultured for 48h.
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Adv Sci (Weinh)
The Novel Dual GIP and GLP-1 Receptor Agonist Tirzepatide Attenuates Colon Cancer Development by Regulating Glucose Metabolism. [Abstract]2025 Mar 24:e2411980. PMID: 40125821 -
Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2024 Dec 5:e2410360. PMID: 39639496 -
Adv Sci (Weinh)
Fatty Acid Oxidation-Glycolysis Metabolic Transition Affects ECM Homeostasis in Silica-Induced Pulmonary Fibrosis. [Abstract]2024 Dec 25:e2407134. PMID: 39721015 -
Adv Sci (Weinh)
An Ultrasensitive Biosensor for Probing Subcellular Distribution and Mitochondrial Transport of l-2-Hydroxyglutarate. [Abstract]2024 Jul 15:e2404119. PMID: 39005231 -
Cell Rep Med
Hypothalamic malate dehydrogenase 2 modulates systemic glucose metabolism through oxytocin-mediated thermogenesis. [Abstract]2026 Feb 17;7(2):102616. PMID: 41672064 -
Cell Death Dis
Cephalomannine inhibits hypoxia-induced cellular function via the suppression of APEX1/HIF-1α interaction in lung cancer. [Abstract]2021 May 14;12(5):490. PMID: 33990544 -
Phytomedicine
Liensinine sensitizes colorectal cancer cells to oxaliplatin by targeting HIF-1α to inhibit autophagy. [Abstract]2024 Jul:129:155647. PMID: 38703660 -
J Hazard Mater
An fusaric acid-based CRISPR library screen identifies MDH2 as a broad-spectrum regulator of Fusarium toxin-induced cell death. [Abstract]2024 Sep 23:480:135937. PMID: 39342847 -
Acta Pharmacol Sin
YY1/HIF-1α/mROS positive-feedback loop exacerbates glomerular mesangial cell proliferation in mouse early diabetic kidney disease. [Abstract]2025 Jul;46(7):1974-1989. PMID: 40038466 -
J Transl Med
Ubiquitin-specific protease 7 maintains c-Myc stability to support pancreatic cancer glycolysis and tumor growth. [Abstract]2024 Dec 20;22(1):1135. PMID: 39707401 -
Dev Cell
2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405 -
Chin Med J (Engl)
Kaempferide inhibited progression of osteoarthritis by targeting the HIF-1 signaling pathway. [Abstract]2025 Sep 17. PMID: 40960306 -
Oncogene
GPER-mediated stabilization of HIF-1α contributes to upregulated aerobic glycolysis in tamoxifen-resistant cells. [Abstract]2023 Jan;42(3):184-197. PMID: 36400971 -
Antioxidants (Basel)
Hypoxia-Inducible Factor 1α Affects Yak Oocyte Maturation and Early Embryonic Development by Regulating Autophagy. [Abstract]2024 Jul 14;13(7):840. PMID: 39061908 -
Stem Cell Res Ther
MSC-exosomes pretreated by Danshensu extracts pretreating to target the hsa-miR-27a-5p and STAT3-SHANK2 to enhanced antifibrotic therapy. [Abstract]2025 Feb 4;16(1):40. PMID: 39901236 -
Aging Cell
Sirtuin 3 reinforces acylcarnitine metabolism and maintains thermogenesis in brown adipose tissue of aging mice. [Abstract]2024 Dec;23(12):e14332. PMID: 39348266 -
Chin Med
Trachelogenin alleviates osteoarthritis by inhibiting osteoclastogenesis and enhancing chondrocyte survival. [Abstract]2024 Mar 1;19(1):37. PMID: 38429848 -
Redox Rep
HIF1A/BNIP3 pathway affects ferroptosis in sepsis-induced cardiomyopathy through binding to BCL-2. [Abstract]2025 Dec;30(1):2544412. PMID: 40779707 -
J Ethnopharmacol
Enhancement of endometrial receptivity by Bushen Zhuyun Decoction via cryptotanshinone-mediated TRIM28 induction and HIF-1α suppression. [Abstract]2025 May 29:119943. PMID: 40449692 -
J Agric Food Chem
2025 Oct 22;73(42):26621-26632. PMID: 41070744 -
Biomater Adv
Synergistic enhancement of desferrioxamine and strontium-doped hydroxyapatite via coaxial electrostatic spinning on osteogenic differentiation. [Abstract]2025 May 27:176:214342. PMID: 40440989 -
Ocul Surf
IL-24 regulates corneal inflammation and fibrosis in fungal keratitis via the caspase-11/gasdermin D pathway. [Abstract]2026 Jan 21:40:12-21. PMID: 41577293 -
Ecotoxicol Environ Saf
Manganese overexposure results in ferroptosis through the HIF-1α/p53/SLC7A11 pathway in ICR mouse brain and PC12 cells. [Abstract]2024 May 22:279:116481. PMID: 38788562 -
Biochem Pharmacol
Dihydroartemisinin breaks the positive feedback loop of YAP1 and GLUT1-mediated aerobic glycolysis to boost the CD8+ effector T cells in hepatocellular carcinoma. [Abstract]2024 May 14:225:116294. PMID: 38754557 -
Life Sci
STC-1 improves scar remodeling and is associated with PI3K/AKT signaling and immune modulation. [Abstract]2026 Mar 15:389:124253. PMID: 41644046 -
Food Funct
Oral exposure to ovalbumin alters glucose metabolism in sensitized mice: upregulation of HIF-1α-mediated glycolysis. [Abstract]2025 Jan 20;16(2):628-639. PMID: 39711353 -
Eur J Pharmacol
2023 Sep 5:954:175858. PMID: 37356787 -
Eur J Pharmacol
Endothelial progenitor cell-derived exosomes inhibit pulmonary artery smooth muscle cell in vitro proliferation and resistance to apoptosis by modulating the Mitofusin-2 and Ras-Raf-ERK1/2 signaling pathway. [Abstract]2023 Jun 15:949:175725. PMID: 37068578
LW6 purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Jun 15:949:175725. [Abstract]
LW6 (10 μM; 48 h) reverses the hypoxia-induced decreased expression of Mfn2 and increased expression of HIF-1α in PASMCs.
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Eur J Pharmacol
The hypoxia-inducible factor 1 inhibitor LW6 mediates the HIF-1α/PD-L1 axis and suppresses tumor growth of hepatocellular carcinoma in vitro and in vivo. [Abstract]2022 Sep 5:930:175154. PMID: 35868447 -
Int Immunopharmacol
HIF-1α drives pyroptosis in extravillous trophoblasts by suppressing PPAR-γ to activate the NLRP3 inflammasome in RA-complicated pregnancy. [Abstract]2026 Jun 1:178:116522. PMID: 41886921 -
Biomolecules
Hypoxia Regulates the Proliferation and Apoptosis of Coronary Artery Smooth Muscle Cells Through HIF-1α Mediated Autophagy in Yak. [Abstract]2025 Feb 10;15(2):256. PMID: 40001559 -
Int J Mol Sci
Hif1α/Dhrs3a Pathway Participates in Lipid Droplet Accumulation via Retinol and Ppar-γ in Fish Hepatocytes. [Abstract]2023 Jun 16;24(12):10236. PMID: 37373386 -
J Cyst Fibros
Cystic fibrosis airway epithelial cells have an exaggerated response to hypoxia that is partially reversible through transmembrane receptor modulation. [Abstract]2025 Aug 15:S1569-1993(25)01561-9. PMID: 40816946 -
Invest Ophthalmol Vis Sci
HIF-1α Promotes Inflammatory Responses in Aspergillus Fumigatus Keratitis by Activating Pyroptosis Through Caspase-8/GSDMD Pathway. [Abstract]2025 Jun 2;66(6):32. PMID: 40492985 -
Arthritis Res Ther
2025 Sep 26;27(1):180. PMID: 41013704 -
Front Cell Dev Biol
Lack of MOF Decreases Susceptibility to Hypoxia and Promotes Multidrug Resistance in Hepatocellular Carcinoma via HIF-1α. [Abstract]2021 Sep 1;9:718707. PMID: 34540836 -
Chem Biol Interact
Oridonin exposure induces testicular impairment through regulating ferroptosis via HIF-1α/HO-1 activation and STUB1-driven GPX4 ubiquitination-dependent degradation. [Abstract]2026 Jan 5:423:111838. PMID: 41265811 -
Mediators Inflamm
Qingxin Lianzi Yin Improves Chronic Kidney Disease by Targeting Ferroptosis via the TLR4/HIF-1α Pathway. [Abstract]2026;2026(1):e7440641. PMID: 42244400 -
Transl Oncol
Loss of the RAGE function in hypoxic conditions exacerbates the malignant progression of lung adenocarcinoma via damage-associated molecular pattern signaling. [Abstract]2026 Jun 18:71:102847. PMID: 42314516 -
Sci Rep
Enhancement of melanoma aggressiveness via p38-MAPK, HIF-1α pathways, and metabolic reprogramming induced by Candida albicans. [Abstract]2025 Nov 17;15(1):40227. PMID: 41249785 -
Cell Signal
Regulatory effects of HIF-1α and HO-1 in hypoxia-induced proliferation of pulmonary arterial smooth muscle cells in yak. [Abstract]2021 Nov:87:110140. PMID: 34478827 -
J Neurochem
Neuronal TRPV1-CGRP axis regulates peripheral nerve regeneration through ERK/HIF-1 signaling pathway. [Abstract]2025 Jan;169(1):e16281. PMID: 39792906 -
Biomedicines
HIF-1α Promotes Macrophage Extracellular Trap Formation and Exacerbates Acute Lung Injury in Neonatal Sepsis. [Abstract]2026 May 18;14(5):1145. PMID: 42193470 -
Biomedicines
Involvement of Lgals3/Galectin-3 in Choroidal Neovascularization and Subretinal Fibrosis Formation. [Abstract]2024 Nov 20;12(11):2649. PMID: 39595213 -
iScience
Canagliflozin attenuates lipotoxicity in cardiomyocytes and protects diabetic mouse hearts by inhibiting the mTOR/HIF-1α pathway. [Abstract]2021 May 7;24(6):102521. PMID: 34142035 -
Front Physiol
Notch3 Modulates Cardiac Fibroblast Proliferation, Apoptosis, and Fibroblast to Myofibroblast Transition via Negative Regulation of the RhoA/ROCK/Hif1α Axis. [Abstract]2020 Jun 30;11:669. PMID: 32695015 -
Vet Res
Neospora caninum hijacks host PFKFB3-driven glycolysis to facilitate intracellular propagation of parasites. [Abstract]2025 Apr 30;56(1):94. PMID: 40307939 -
Exp Cell Res
Silencing of LOX-1 attenuates high glucose-induced ferroptosis in THVECs via the HIF-1α/SLC7A11 signaling pathway. [Abstract]2025 Mar 15;446(2):114451. PMID: 40015503 -
Exp Eye Res
PCBP1 modulates cellular iron homeostasis via targeting HIF-1α/HO-1 pathway and alleviates high-glucose-induced ferroptosis in HRMECs. [Abstract]2025 Oct:259:110576. PMID: 40789503 -
Genes (Basel)
Donkey Oil-Based Ketogenic Diet Prevents Tumor Progression by Regulating Intratumor Inflammation, Metastasis and Angiogenesis in CT26 Tumor-Bearing Mice. [Abstract]2023 Apr 30;14(5):1024. PMID: 37239383 -
Toxicol In Vitro
The SNHG10-miR-495-3p-PTEN axis is involved in sevoflurane-mediated protective effects in cardiomyocytes against hypoxia/reoxygenation injury. [Abstract]2024 Feb:94:105724. PMID: 37884162 -
Am J Drug Alcohol Abuse
Regulation of HDL metabolism in alcohol-associated liver disease: the role of HIF-1α and miR-185 in SR-BI suppression. [Abstract]2025 May 27:1-11. PMID: 40423556 -
J Chem Neuroanat
HIF-1α aggravated traumatic brain injury by NLRP3 inflammasome-mediated pyroptosis and activation of microglia. [Abstract]2021 Oct:116:101994. PMID: 34166779 -
Biochem Biophys Res Commun
Hyperuricemia induces liver injury by upregulating HIF-1α and inhibiting arginine biosynthesis pathway in mouse liver and human L02 hepatocytes. [Abstract]2022 Aug 30;617(Pt 2):55-61. PMID: 35696777 -
J Appl Genet
Interaction between CA repeat microsatellites and HIF1α regulated the transcriptional activity of porcine IGF1 promoter. [Abstract]2020 Feb;61(1):105-112. PMID: 31673965
LW6 purchased from MedChemExpress. Usage Cited in: J Appl Genet. 2020 Feb;61(1):105-112. [Abstract]
The protein expression level of HIF1α was detected throughWestern blot analysis 48 h after treatment of LW6.
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Oxid Med Cell Longev
The ROS/GRK2/HIF-1 α/NLRP3 Pathway Mediates Pyroptosis of Fibroblast-Like Synoviocytes and the Regulation of Monomer Derivatives of Paeoniflorin. [Abstract]2022 Jan 29:2022:4566851. PMID: 35132350
Solvent & Solubility
DMSO : 25 mg/mL (57.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 17.24 mg/mL (39.59 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.74 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: The mice receive the following treatments using a dosing vehicle solution, containing 10% dimethylacetamide, 10% Cremophor EL and 80% of sodium carbonate buffer (pH 10), by intraperitoneal (i.p.) injection: group1(control group; six mice), vehicle solution; group2 (six mice), LW6 at a dose of 10 and 20mg/kg (QD); and group 3 (six mice), topotecan at a dose of 2mg/kg, (Q2D), which is the dose and dosing schedule that showed more than 60% inhibition of growth of HCT116 tumors. The treatments are continued for 13 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Naik R, et al. Synthesis and structure-activity relationship study of chemical probes as hypoxia induced factor-1α/malate dehydrogenase 2 inhibitors. J Med Chem. 2014 Nov 26;57(22):9522-38. [Content Brief]
[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. [Content Brief]
[3]. Song JG, et al. Discovery of LW6 as a new potent inhibitor of breast cancer resistance protein. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 2.2962 mL | 11.4808 mL | 22.9616 mL | 57.4040 mL |
| 5 mM | 0.4592 mL | 2.2962 mL | 4.5923 mL | 11.4808 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2962 mL | 5.7404 mL | |
| 15 mM | 0.1531 mL | 0.7654 mL | 1.5308 mL | 3.8269 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1481 mL | 2.8702 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9185 mL | 2.2962 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9135 mL | |
| DMSO | 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4351 mL |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL |
LW6 Related Classifications
HY-13671 Related Classifications
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