HKC54
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.
- Formula: C18H20N2O5
- Molecular Weight:344.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
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TRPV2 0.4 μM (IC50) |
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.
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.
Chemical Information
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Molecular Weight 344.36
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Formula C18H20N2O5
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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
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HKC54 Related Classifications
HY-182896 Related Classifications
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