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  1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP RIP kinase Apoptosis Necroptosis
  3. Kongensin A

Kongensin A 是一種從 Croton kongensis 中分離的天然產(chǎn)物。 Kongensin A 是一種有效的,共價的 HSP90 抑制劑,可阻斷 RIP3 依賴性壞死病。Kongensin A 是一種有效的壞死性抑制劑和凋亡誘導劑,并具有潛在的抗壞死性和消炎性應用。

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Kongensin A Chemical Structure

Kongensin A Chemical Structure

CAS No. : 885315-96-8

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications[1].

IC50 & Target

HSP90[1]
RIP3[1]
Apoptosis[1]

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
0.12 μM
Compound: 8
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
[PMID: 34236840]
MDA-MB-231 IC50
0.177 μM
Compound: 8
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
[PMID: 34236840]
MDA-MB-468 IC50
0.228 μM
Compound: 8
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
[PMID: 34236840]
體外研究
(In Vitro)

Kongensin A (0-15 μM;6 小時;HT29 細胞) 處理以劑量依賴性方式在多種癌細胞系中誘導 caspase 激活和細胞凋亡[1]。
Kongensin A (0 -15 μM;24 hours;HT29細胞) 處理誘導 RIPK1 和致癌激酶如 ERBB2、AKT、EGFR 和 B-raf 的降解,并誘導 HSP90A 和 HSP90B 的上調(diào)[1]。
Kongensin A 共價結合 HSP90 中間結構域的半胱氨酸 420,并將 HSP90 與其輔伴侶 CDC37 解離。RIP3 激活需要 HSP90-CDC37 復合物,KA 阻斷 LPS/Smac 模擬物/Z-VAD 和 RIP3 聚合誘導的細胞死亡,其中細胞死亡依賴于 RIP3 而不是其上游激酶 RIP1[1]。

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

Apoptosis Analysis[1]

Cell Line: HT29 cells
Concentration: 0 μM, 2.5 μM, 5 μM, 15 μM
Incubation Time: 6 hours
Result: Induced caspase activation and apoptosis in a dosage-dependent manner.

Western Blot Analysis[1]

Cell Line: HT29 cells
Concentration: 0 μM, 2.5 μM, 5 μM, 15 μM
Incubation Time: 24 hours
Result: Induced the degradation of RIPK1 and oncogenic kinases such as ERBB2, AKT, EGFR, and B-raf, and induced the up-regulation of HSP90A and HSP90B.
分子量

374.47

Formula

C22H30O5

CAS 號
性狀

固體

顏色

White to light yellow

初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

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

純度 & 產(chǎn)品資料

純度: ≥98.0%

參考文獻
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  • 稀釋計算器

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

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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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產(chǎn)品名稱:
Kongensin A
目錄號:
HY-N3417
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