Product Details
| Product Name:
LW6 |
CAS No.:
934593-90-5 |
| Purity:
99.10% |
Supply Ability:
10g |
| Release date:
2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | LW6 |
| 描述 | LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor. |
| 細(xì)胞實驗 | 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]. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | 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]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (114.81 mM)
|
| 關(guān)鍵字 | LW 6 | Apoptosis | Hypoxia-inducible factors | inhibit | HIF-PH | HIF/HIF Prolyl-Hydroxylase | CAY-10585 | LW6 | LW-6 | HIFs | LW 8 | Inhibitor | LW-8 | HIF-1alpha inhibitor | HIF-1a inhibitor | CAY 10585 |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Glucosamine | Hydroxycitric acid tripotassium hydrate |
| 相關(guān)庫 | 糖代謝化合物庫 | 經(jīng)典已知活性庫 | 谷氨酰胺代謝化合物庫 | 抑制劑庫 | 干細(xì)胞分化化合物庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 轉(zhuǎn)錄因子庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
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Suppliers |
Update time |
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$1.00/1g |
VIP5Y
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Career Henan Chemical Co
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2019-12-23 |
United States