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].
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].
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].
References:
[1]. Kiely-Collins H, et al. Selective TRPV2 Antagonists Derived from the Natural Product Piperlongumine Inhibit Cancer Cell Migration and Metastasis. ACS Chem Biol. 2026;21(4):674-688.
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].
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].
References:
[1]. Kiely-Collins H, et al. Selective TRPV2 Antagonists Derived from the Natural Product Piperlongumine Inhibit Cancer Cell Migration and Metastasis. ACS Chem Biol. 2026;21(4):674-688.