1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. Diazepinomicin

Diazepinomicin  (Synonyms: ECO-4601; TLN-4601; BU 4664L)

目录号: HY-N6674
COA 产品使用指南 技术支持

Diazepinomicin (TLN-4601) 是Micromonospora sp 的次生代谢产物,可抑制EGF 诱导的 Ras-ERK MAPK 信号通路,可诱导凋亡。是一种可用于 K-Ras 突变型的抗肿瘤活性分子。

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Diazepinomicin Chemical Structure

Diazepinomicin Chemical Structure

CAS No. : 733035-26-2

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查看 Ras 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

Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models[1].

IC50 & Target

Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway post Ras prenylation and prior to MEK activation[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HUVEC IC50
0.43 μg/mL
Compound: 1, BU-4664L
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
Antiinvasive activity against HUVEC assessed as inhibition of cell migration after 6 hrs by Matrigel assay
[PMID: 20056543]
HUVEC IC50
0.72 μg/mL
Compound: 1, BU-4664L
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
Antiangiogenic activity against HUVEC cells assessed as inhibition of vascular formation after 6 hrs by wound healing assay
[PMID: 20056543]
NCI-H460 GI50
13.6 μM
Compound: 1; BU-4664L
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay
[PMID: 34838651]
PC-3 GI50
1.95 μM
Compound: 1; BU-4664L
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition by MTT assay
[PMID: 34838651]
Renca IC50
0.78 μg/mL
Compound: 1, BU-4664L
Antiinvasive activity against mouse Renca by Matrigel assay
Antiinvasive activity against mouse Renca by Matrigel assay
[PMID: 20056543]
Clinical Trial
分子量

462.58

Formula

C28H34N2O4

CAS 号
性状

固体

颜色

Off-white to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

纯度 & 产品资料
参考文献
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  • 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 *
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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:
Diazepinomicin
目录号:
HY-N6674
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