HKC54
Based on 1 Customer Validation
HKC54 is a selective TRPV2 antagonist with an IC50 of 0.4 μM. HKC54 binds directly to TRPV2 and inhibits TRPV2-mediated calcium influx. HKC54 inhibits glioblastoma cell migration in vitro and breast cancer metastasis in vivo. HKC54 can be used for the research of breast cancer lung metastasis.
For research use only. We do not sell to patients.
- Purity : 98.49%
- Formula: C18H20N2O5
- Molecular Weight:344.36
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
TRPV2 0.4 μM (IC50) |
In Vitro
HKC54 (5 μM) significantly inhibits TRPV2-mediated calcium influx in hTRPV2-RFP-transfected HEK293T cells when used as a pretreatment prior to CBD stimulation[1].
HKC54 (10 μM) directly engages TRPV2 in MDA-MB-231 cell lysate, as evidenced by significant thermal stabilization of the channel[1].
HKC54 (5-10 μM; up to 60 h) inhibits migration of U-251 WT glioblastoma cells in a TRPV2-dependent manner, with no effect on U-251 TRPV2 KD cells[1].
HKC54 (20 μM; 6 h) does not deplete intracellular GSH levels in MCF-7 breast cancer cells[1].
HKC54 (20 μM; 4 h) does not induce reactive oxygen species in MCF-7 breast cancer cells[1].
HKC54 (1-100 μM; 48 h) does not reduce cell viability of U-251 WT or U-251 TRPV2 KD glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-251 wild-type (WT) glioblastoma cells, U-251 TRPV2 knockdown (KD) glioblastoma cells
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Concentration:5 μM, 10 μM (treatment for up to 60 h)
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Incubation Time:up to 60 h
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Result:Inhibited cell migration significantly in U-251 WT cells at both 5 μM and 10 μM compared to DMSO control.
Had no significant effect on migration in U-251 TRPV2 KD cells.
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Cell Line:U-251 glioblastoma cells, U-251 TRPV2 KD glioblastoma cells
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Concentration:1-100 μM (treatment for 48 h)
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Incubation Time:48 h
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Result:Did not significantly reduce cell viability in either U-251 WT or U-251 TRPV2 KD cells, unlike PL which caused a concentration-dependent reduction in viability.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice[1]
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Dosage:12.5 mg/kg; 25 mg/kg
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Administration:every other day; 5 doses
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Result:Did not cause body weight loss in mice.
Produced a marked reduction in lung metastatic nodules relative to vehicle control.
Nearly eliminated detectable lung nodules at 25 mg/kg dose.
- Scratch/Wound-Healing Migration Assay
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Ca2+ Staining Technique
- Breast Cancer Modeling
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Tail-Vein Experimental Metastasis Xenograft
- 3D Collagen/Hydrogel Matrix Migration Assay
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Orthotopic Cell-Line Xenograft
Chemical Information
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Appearance Solid
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Molecular Weight 344.36
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Formula C18H20N2O5
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Color White to off-white
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SMILES
COC1=CC(/C=C(C(N2CCCCC2=O)=O)\C#N)=CC(OC)=C1OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (145.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9039 mL | 14.5197 mL | 29.0394 mL | 72.5984 mL |
| 5 mM | 0.5808 mL | 2.9039 mL | 5.8079 mL | 14.5197 mL | |
| 10 mM | 0.2904 mL | 1.4520 mL | 2.9039 mL | 7.2598 mL | |
| 15 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL | 4.8399 mL | |
| 20 mM | 0.1452 mL | 0.7260 mL | 1.4520 mL | 3.6299 mL | |
| 25 mM | 0.1162 mL | 0.5808 mL | 1.1616 mL | 2.9039 mL | |
| 30 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4199 mL | |
| 40 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL | 1.8150 mL | |
| 50 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4520 mL | |
| 60 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 80 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9075 mL | |
| 100 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7260 mL |
HKC54 Related Classifications
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