Cat.No. : CSC-RG01852 Host Cell: HEK293
| Cat. No. | CSC-RG01852 |
| Description | This cell line is engineered to stably overexpress human MC1R in HEK293 cells. |
| Gene | MC1R |
| Gene Species | Homo sapiens (Human) |
| Host Cell | HEK293 |
| Host Cell Species | Homo sapiens (Human) |
| Stability | This cell line is stable at least 10 passages. |
| Product Type | Stable cell line constitutively expressing human kinase gene(s) |
| Applications | HEK293 stable cell lines expressing GPCR genes have a wide range of uses in basic research and drug discovery. 1) High - throughput Screening: These cell lines are widely used in high - throughput screening assays to identify new ligands for GPCRs. By exposing the cells to large libraries of small molecules or other compounds and monitoring the resulting cellular responses, potential drug candidates can be rapidly identified. 2) Drug Target Validation: They provide a valuable tool for validating GPCRs as drug targets. Researchers can study the effects of specific drugs or genetic manipulations on the GPCR - expressing cells to assess the functional significance of the GPCR in a particular biological process. This helps to determine whether targeting a specific GPCR is likely to have therapeutic benefits. 3) Pharmacological Characterization: HEK293 stable cell lines allow for the detailed pharmacological characterization of GPCR ligands. Parameters such as binding affinity, efficacy, and potency can be determined by measuring the ligand - induced responses in these cells. This information is crucial for optimizing the design of new drugs and understanding their mechanism of action. |
| Quality Control | 1) Real-time qPCR analysis of gene mRNA overexpression level 2) Analysis of GPCR function by cAMP assay 3) mycoplasma detection |
| Size Form | One vial of frozen cells, typically >1x10^6cells/vial |
| Shipping | Dry ice |
| Storage | Liquid nitrogen |
| Revival | Rapidly thaw cells in a 37°C water bath. Transfer contents into a tube containing pre-warmed media. Centrifuge cells and seed into a 25 cm2 flask containing pre-warmed media. |
| Growth Properties | Adherent |
| Mycoplasma | Negative |
| Format | One frozen vial containing millions of cells |
| Storage | Liquid nitrogen |
| Safety Considerations |
The following safety precautions should be observed. 1. Use pipette aids to prevent ingestion and keep aerosols down to a minimum. 2. No eating, drinking or smoking while handling the stable line. 3. Wash hands after handling the stable line and before leaving the lab. 4. Decontaminate work surface with disinfectant or 70% ethanol before and after working with stable cells. 5. All waste should be considered hazardous. 6. Dispose of all liquid waste after each experiment and treat with bleach. |
| Ship | Dry ice |
Melanoma is a deadly skin cancer. Despite recent breakthroughs with BRAF-V600E and PD-1 inhibitors showing significant clinical efficacy, melanoma can ultimately develop resistance to these targeted therapies. To address this resistance problem, researchers designed and synthesized a ligand-drug conjugate that couples a cytotoxic drug with low resistance potential to the melanocortin 1 receptor (MC1R) agonist melanocortin-II (MT-II), thereby targeting melanoma cells that overexpress MC1R. In vitro experiments showed that the drug-MT-II conjugate maintained strong binding to MC1R and achieved selective drug delivery to A375 melanoma cells through its MT-II portion. Furthermore, using camptothecin as the cytotoxic drug, camptothecin-MT-II (compound 1) effectively inhibited the growth of A375 melanoma cells with an IC50 value of 16 nM. By conferring melanoma cell selectivity through its MT-II portion, this drug-MT-II conjugate approach allows for a wider selection of cytotoxic drugs, which may be key to overcoming melanoma drug resistance.
To evaluate the binding affinity of compounds 1 and 2 to MC1R, researchers performed competitive binding experiments using human MC1R overexpressing HEK293 cells and 125I-labeled NDP-α-MSH as a competitive ligand (Figure 1, Table 1). The Ki values for CPT-MT-II and fluorescein-labeled MT-II binding to MC1R were determined to be 57 ± 7 nM and 172 ± 20 nM, respectively, while the Ki value for MT-II was 1.5 ± 0.2 nM. Although the binding affinity was lower than that of MT-II, compounds 1 and 2 were able to completely displace 125I-NDP-α-MSH in the micromolar concentration range. Since MT-II is not selective for MC1R and can also bind to and activate other melanocortin receptor subtypes, the researchers further conducted competitive binding experiments using HEK293 cells overexpressing MC3R, MC4R, or MC5R. The results showed that CPT-MT-II exhibited some selectivity for MC1R, with its binding affinity to MC1R being approximately 3-6 times higher than its binding affinity to MC3R, MC4R, and MC5R (Table 1).
Figure 1. Competitive binding assay results of MT-II, CPT-MT-II 1 and
fluorescein-MT-II 2 binding to MC1R in competition with 125I labeled NDP-α-MSH. ( Zhou Y, et
al., 2020)
Table 1. Ki Values of MT-II, CPT-MT-II and Fluorescein-MT-II Binding to Melanocortin Receptors.
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The Human MC1R Stable Cell Line - HEK293 delivers clear, reproducible dose-response curves with minimal variability. We saw stable receptor expression over multiple weeks, enabling confident comparisons across studies.
This MC1R stable line from Creative Biogene has been a game-changer for our pigmentation pathway research. The background noise in our cAMP accumulation assays was incredibly low, allowing us to detect even subtle agonist activities. Highly recommended for functional characterization.
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