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  2. Anti-infection Epigenetics TGF-beta/Smad Apoptosis Autophagy
  3. Beta-lactamase PKC Bcl-2 Family Apoptosis Autophagy
  4. Chelerythrine

Chelerythrine  (Synonyms: 白屈菜紅堿)

目錄號: HY-N2359
產(chǎn)品使用指南

Chelerythrine 是一種天然生物堿，為有效、選擇性的 Ca2+/磷脂依賴性 PKC 拮抗劑，IC50 值為 0.7 μM。Chelerythrine 具有抗腫瘤、抗糖尿病、抗炎的活性。Chelerythrine 抑制 BclXL-Bak BH3 肽結(jié)合，IC50 為 1.5 μM，并從 BclXL 取代了 Bax。 Chelerythrine 誘導(dǎo)細(xì)胞凋亡和自噬。

在相同的摩爾濃度下，化合物鹽形式與游離形式有相同的生物活性，但鹽形式 Chelerythrine chloride 通常具有更好的水溶性和穩(wěn)定性。

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Chelerythrine Chemical Structure

Chelerythrine Chemical Structure

CAS No. : 34316-15-9

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Chelerythrine 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of Chelerythrine:

    Chelerythrine purchased from MCE. Usage Cited in: Sci Rep. 2017 Aug 23;7(1):9201.  [Abstract]

    CGP3466B upregulates PCMT1 expression and inhibits cleaved-Mst1 activation at 24?h after TBI. Chelerythrine activates the Mst1 without regulating PCMT1 protein level. (a) Western blot assay for the expression of PCMT1. (b) Western blot assay for the expression of Mst1 and cleaved-Mst1.

    查看 Beta-lactamase 亞型特異性產(chǎn)品:

    查看 PKC 亞型特異性產(chǎn)品:

    查看 Bcl-2 Family 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity[2]. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy[3][4].

    IC50 & Target[1]

    PKC

    0.7 μM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    7.73 μM
    Compound: Chelerythrine
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    HUVEC IC50
    4.93 μM
    Compound: Chelerythrine
    Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against HUVEC assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    MKN-45 IC50
    12.7 μM
    Compound: Chelerythrine
    Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    		[PMID: 27887841]
    NB-4 IC50
    1.49 μM
    Compound: Chelerythrine
    Cytotoxicity against human NB4 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human NB4 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    		[PMID: 27887841]
    NCI-H1299 IC50
    4.28 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H1299 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    NCI-H292 IC50
    4.96 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H292 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    NCI-H460 IC50
    5.14 μM
    Compound: Chelerythrine
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 27561984]
    體外研究
    (In Vitro)

    Chelerythrine (48 小時) 抑制 L-1210 細(xì)胞的生長 (IC50: 0.53 uM)[1]。
    Chelerythrine (0-20 μM，24 小時) 可抑制 A549 和 NCI-H1299 細(xì)胞的細(xì)胞活力，誘導(dǎo)細(xì)胞凋亡和自噬[4]。
    Chelerythrine (0-5 μM，24 或 48 小時) 可誘導(dǎo) BclXL 過表達(dá)的 SH-SY5Y 細(xì)胞凋亡[3]。
    Chelerythrine (2.5-10 μM，16 小時) 可誘導(dǎo) SH-SY5Y 細(xì)胞線粒體去極化 (線粒體電位降低)，并刺激分離的線粒體釋放 CytC[4]。
    Chelerythrine (0-100 ng/mL，24 小時) 可減少 LPS 誘導(dǎo)的原代巨噬細(xì)胞中 NO 和 TNF-α 的產(chǎn)生[5]。
    Chelerythrine (MIC: 0.156 mg/mL) 對革蘭氏陽性菌、金黃色葡萄球菌 (SA)、MRSA 和超廣譜 β-內(nèi)酰胺酶金黃色葡萄球菌 (ESBLs-SA) 具有抗菌活性[6]。

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

    Western Blot Analysis[4]

    Cell Line: A549 and NCI-H1299 cells
    Concentration: 10, 15, 20 μM
    Incubation Time: 24 h
    Result: Induced expression of LC3-II in a beclin 1-dependent way.
    體內(nèi)研究
    (In Vivo)

    Chelerythrine (5 mg/kg，腹腔注射，每日) 可減輕新生大鼠中部分單側(cè)輸尿管梗阻 (UUO) 引起的腎損傷，并恢復(fù)腎功能[2]。
    Chelerythrine (1-10 mg/kg，腹腔注射，注射 100 μg/kg LPS 前 24 小時和 1 小時) 在 LPS 誘導(dǎo)的小鼠內(nèi)毒素休克中顯示出抗炎作用 (提高存活率、降低血清亞硝酸鹽和 TNF-α 水平)[5]。

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

    Animal Model: Unilateral ureteral obstruction (UUO) induced neonatal rats[2]
    Dosage: 5 mg/kg
    Administration: i.p., daily
    Result: Attenuated kidney injury (Increased kidney weight and restored renal function).
    Inhibited UUO-induced upregulated kidney injury molecule-1 expression, apoptosis, and renal fibrosis.
    分子量

    348.37

    Formula

    C21H18NO4
    CAS 號
    中文名稱

    白屈菜紅堿；白屈菜赤堿
    結(jié)構(gòu)分類
    初始來源
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

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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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