2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel Calcium Channel
  4. 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.

HKC54

HKC54 Chemical Structure

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HKC54 Related Antibodies

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Description

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[1].

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.

HKC54 Related Antibodies

Cell Migration Assay [1]

Cell Line: U-251 wild-type (WT) glioblastoma cells, U-251 TRPV2 knockdown (KD) glioblastoma cells
Concentration: 5 μM, 10 μM (treatment for up to 60 h)
Incubation Time: up to 60 h
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.

Cell Viability Assay[1]

Cell Line: U-251 glioblastoma cells, U-251 TRPV2 KD glioblastoma cells
Concentration: 1-100 μM (treatment for 48 h)
Incubation Time: 48 h
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

HKC54 (12.5-25 mg/kg; i.p.; every other day; 5 doses) potently inhibits breast cancer lung metastasis in Balb/c mice, with no associated body weight loss, and the 25 mg/kg dose nearly eliminates lung metastatic nodules[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice[1]
Dosage: 12.5 mg/kg; 25 mg/kg
Administration: every other day; 5 doses
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.
Molecular Weight

344.36

Formula

C18H20N2O5
SMILES

COC1=CC(/C=C(C(N2CCCCC2=O)=O)\C#N)=CC(OC)=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HKC54 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HKC54HKC 54HKC-54TRP ChannelCalcium ChannelTransient receptor potential channelsCa2+ channelsCa channelsTRPV1MCF-7 breast cancer cellsHEK293T cellsU-251 TRPV2 KD cellsbreast cancer lung metastasisBalb/c miceTRPV2MDA-MB-231 cell lysateU-251 WT glioblastoma cellsTRPA1Inhibitorinhibitorinhibit

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