1. Metabolic Enzyme/Protease
  2. MMP
  3. cyclo(RLsKDK)

cyclo(RLsKDK)  (Synonyms: BK-1361)

目录号: HY-P1676
产品使用指南

cyclo(RLsKDK) (BK-1361) 是一种特异性的金属蛋白酶 ADAM8 抑制剂,IC50 值为 182 nM。cyclo(RLsKDK) 在炎性疾病和癌症中有潜在应用。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 cyclo(RLsKDK) TFA 通常具有更好的水溶性和稳定性。

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Custom Peptide Synthesis

cyclo(RLsKDK) Chemical Structure

cyclo(RLsKDK) Chemical Structure

CAS No. : 1975145-82-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer[1].

体外研究
(In Vitro)

cyclo(RLsKDK) 促使 ADAM8 激活和 CD23 脱落,IC50 值分别为 120 nM 和 182 nM。
cyclo(RLsKDK) (200 nM;0-120 h) 增加了 pro-ADAM8 的活性[2]
cyclo(RLsKDK) (200 nM and 500 nM;12 h) 促进了 Panc1_ctrl 和 Panc1_A8 细胞的生长[2]
cyclo(RLsKDK) (500 nM) 导致 Panc1_ctrl 和 Panc1_A8 细胞中 ERK1/2 磷酸化[2]

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

Cell Invasion Assay[2]

Cell Line: Panc1_A8 cells.
Concentration: 10, 100 and 1,000 nM.
Incubation Time: 6 h.
Result: Reduced cell invasion with dose-dependent manner.
体内研究
(In Vivo)

cyclo(RLsKDK) (10 µg/g;腹腔注射;一周一次持续 4 周) 显著降低了植入 Panc1_ctrl 或 Panc1_A8 细胞的小鼠中的肿瘤量。cyclo(RLsKDK) 提高了胰腺导管腺癌 (PDAC) 小鼠存活率,降低了可溶性 ADAM8 (sADAM8) 含量、pERK1/2 活化、PDAC 在 PDAC 小鼠肝脏和肺部中的转移[2]

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

分子量

727.85

Formula

C31H57N11O9

CAS 号
Sequence

Cyclo(Arg-Leu-{d-Ser}-Lys-Asp-Lys)

Sequence Shortening

Cyclo(RL-{d-Ser}-KDK)

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
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  • 稀释计算器

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

质量   浓度   体积   分子量 *
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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:
cyclo(RLsKDK)
目录号:
HY-P1676
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