1. Metabolic Enzyme/Protease
  2. Carbonic Anhydrase
  3. CAI/II-IN-12

CAI/II-IN-12 是一种强效的 hCAI (IC50 = 7.12 μM,Ki = 9.26 μM) 和 hCAII (IC50 = 10.62 μM,Ki = 11.72 μM) 双重抑制剂。CAI/II-IN-12 对 CYP17A1、hCAI 和 hCAII 酶的活性位点具有很强的亲和力。CAI/II-IN-12 表现出快速的构象稳定作用,尤其是在 CYP17A1 复合物中。CAI/II-IN-12 可用于前列腺癌治疗和青光眼的研究。

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CAI/II-IN-12

CAI/II-IN-12 Chemical Structure

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Customer Review

查看 Carbonic Anhydrase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CAI/II-IN-12 is a potent and hCAI (IC50 = 7.12 μM, Ki = 9.26 μM) and hCAII (IC50 = 10.62 μM, Ki = 11.72 μM) dual inhibitor. CAI/II-IN-12 has a strong affinity for the active sites of CYP17A1, hCAI, and hCAII enzymes. Compound CAI/II-IN-12 exhibits rapid conformational stabilization, particularly in the CYP17A1 complex. CAI/II-IN-12 can be used for the study of prostate cancer therapy and glaucoma[1].

IC50 & Target

hCA I

7.12 μM (IC50)

hCA II

10.62 μM (IC50)

体外研究
(In Vitro)

CAI/II-IN-12 (Compound 6d) (1-100 μM,24 小时) 对前列腺癌细胞 (DU145) 表现出选择性抑制活性,且对正常细胞 (PNT1a) 毒性较低[1]
CAI/II-IN-12 与 CYP17A1 结合后,其三唑部分的羰基氧与酶 HEM 基团中的中心铁原子之间形成配位键,展现出显著的潜力[1]

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

Cell Viability Assay[1]

Cell Line: DU145 cells, PNT1a cells
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 24 h
Result: In DU145 cancer cells, exhibited dose-dependent inhibition of cell viability.
In normal PNT1a cells, the IC50 value was 113.44 μM, and the selectivity index (SI) was 2.28.
分子量

504.56

Formula

C26H24N4O5S

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:
CAI/II-IN-12
目录号:
HY-175972
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