2. Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. MDM-2/p53 HSP
  4. Colletofragarone A2

Colletofragarone A2 可从真菌 Colletotrichum sp. (13S020) 中分离获得。Colletofragarone A2 抑制 p53 突变蛋白和 HSP90，具有抗癌活性。Colletofragarone A2 能够促进 p53 突变蛋白降解和聚合，并抑制体内肿瘤生长。

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Colletofragarone A2 Chemical Structure

Colletofragarone A2 Chemical Structure

CAS No. : 181377-06-0

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Colletofragarone A2 相关抗体

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo[1].

IC50 & Target

HSP90

 

体外研究
(In Vitro)

Mutant p53 loses original tumor suppressor function but acquires new abilities regarding oncogenic progression[1].
Colletofragarone A2 (0.05-5 μM; 72 h) shows high selectivity and more cytotoxic activity on cells with p53R175H structural mutants than with other p53 statuses such as a DNA-contact mutant, wild-type, and null cells[1].
Colletofragarone A2 (2 μM; 8 h) decreases mutant p53 levels in SK-BR-3 (p53R175H) cells by promoting p53 degradation[1].
Colletofragarone A2, combinded with 10 μM MG-132 (HY-13259), (2 or 4 μM; 4 h) induces the accumulation of the aggregated mutant p53[1].

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

Colletofragarone A2 相关抗体:

Western Blot Analysis[1]

Cell Line: SK-BR-3 (p53R175H), HuCCT1 (p53R175H), Saos-2 (p53R175H), OVCAR-3 (p53R248Q), and A549 (wild-type p53)
Concentration: 0, 0.5, 1, 2, 4 μM
Incubation Time: 4 hours
Result: Decreased the mutant p53R175H levels in SK-BR-3 and HuCCT1 cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: SK-BR-3 (p53R175H) cells
Concentration: 2 μM, 4 μM (with 10 μM MG-132 (HY-13259), respectively)
Incubation Time: 4 hours
Result: Promoted the proteasome-mediated degradation of mutant p53 and the accumulation of precipitated mutant p53.

Cell Viability Assay[1]

Cell Line: SK-BR-3 (p53R175H), HuCCT1 (p53R175H), OVCAR-3 (p53R248Q), and A549 (wild-type p53) cells
Concentration: 0.05-5 μM
Incubation Time: 72 hours
Result: Decreased the level of p53 and showed high selectivity and more cytotoxic activity on cells with p53R175H structural mutants, IC50s of 0.18 μM (SK-BR-3), 0.35 μM (HuCCT1), respectively.
体内研究
(In Vivo)

Colletofragarone A2 (0.35 mM, 100 μL; injected intratumorally and daily; 13 d) markedly decreases tumor cell growth in mouse infected with HuCCT1 (p53R175H) cells[1].

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

Animal Model: Xenograft model with HuCCT1 (p53R175H) cells in mouse[1]
Dosage: 0.35 mM with 100 μL (DMSO solution)
Administration: Injected intratumorally; daily; 13 days; tested tumor growth at 1, 3, 5, 7, 9, 13 days
Result: Inhibited tumor growth without lowing body weight of mouse.
分子量

386.44

Formula

C22H26O6
CAS 号
结构分类
初始来源

Colletotrichum sp.
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

Colletofragarone A2 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Colletofragarone A2181377-06-0Colletofragarone A 2Colletofragarone A-2MDM-2/p53HSPHeat shock proteinsColletotrichum13S020degradationaggregationmutant p53p53R175H?structural mutantsHuCCT1SK-BR-3molecular chaperoneMG-132Inhibitorinhibitorinhibit

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