1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel Calcium Channel
  3. HKC54

HKC54 是一种选择性的 TRPV2 拮抗剂,IC50 为 0.4 μM。HKC54 可直接与 TRPV2 结合抑制 TRPV2 介导的钙内流。HKC54 可在体外抑制胶质母细胞瘤细胞迁移,在体内抑制乳腺癌转移。HKC54 可用于乳腺癌肺转移的研究。

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HKC54

HKC54 Chemical Structure

1.  客户无需承担相应的运输费用。

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     可免费申领三个不同产品的试用装。

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

HKC54 (5 μM) 可显著抑制 hTRPV2-RFP 转染的 HEK293T 细胞中 TRPV2 介导的钙内流[1]
HKC54 (10 μM) 在 MDA-MB-231 细胞裂解物中直接结合 TRPV2,这一点可通过该通道显著的热稳定性得到证明[1]
HKC54 (5-10 μM; up to 60 h) 以 TRPV2 依赖的方式抑制 U-251 WT 胶质母细胞瘤细胞的迁移,而对 U-251 TRPV2 KD 细胞无影响[1]
HKC54 (20 μM; 6 h) 不会消耗 MCF-7 乳腺癌细胞内的 GSH 水平[1]
HKC54 (20 μM; 4 h) 不会在 MCF-7 乳腺癌细胞中诱导活性氧生成[1]
HKC54 (1-100 μM; 48 h) 不会降低 U-251 WT 或 U-251 TRPV2 KD 胶质母细胞瘤细胞的活力[1]

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

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.
体内研究
(In Vivo)

HKC54 (12.5-25 mg/kg;每隔 1 天给 1 次;共 5 次) 可强效抑制 Balb/c 小鼠的乳腺癌肺转移,且未引发体重下降[1]

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.
分子量

344.36

Formula

C18H20N2O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
HKC54
目录号:
HY-182896
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