Shikonin (C.I. 75535)

For research use only. Not for use in humans.

製品コードS8279 別名:Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844

Shikonin (C.I. 75535)化学構造

CAS No. 54952-43-1

Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

サイズ 価格(税別)  
JPY 18100
JPY 51300
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

製品安全説明書

PKM阻害剤の選択性比較

生物活性

製品説明 Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
ターゲット
chemokine receptor [1]
()
TNF-α [4]
()
Proteasome [4]
()
NF-κB [1]
()
PKM2 [3]
(FBP absence)
0.3 μM
体外試験

At nanomolar concentrations, shikonin inhibits monocyte chemotaxis and calcium flux in response to a variety of CC chemokines (CCL2 [monocyte chemoattractant protein 1], CCL3 [macrophage inflammatory protein 1α], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1α]), and classic chemoattractants (formylmethionyl-leucine-phenylalanine and complement fraction C5a). Shikonin down-regulates surface expression of CCR5, a primary HIV-1 coreceptor, on macrophages. The anti-HIV and anti-inflammatory activities of shikonin may be related to its interference with chemokine receptor expression and function[1]. Shikonin inhibits enterocyte calcium-activated chloride channels, the inhibitory effect is partially through inhibition of basolateral K+ channel activity[2].

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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TE-441-T NUXkNIxwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;lZ5NxUW6qaXLpeIlwdiCxZjDoeY1idiCWRT20OFEuXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMECyNlM5|ryPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
NALM-6 MlW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHhVZN2UW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByMke5O:69VS5? NYLQV4RYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
SW1710 NVfYWlVCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV3n[ZEyUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByMkmx{txONg>? NVXG[ZpyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
Bcl2 / Bax / CytC / Apaf1 / AIF / Caspase-9 / Caspase-3 / Caspase-7 ; 

PubMed: 25879420     


Shikonin treatment alters expression of mitochondrial proteins in DU-145 and PC-3 cells. Cells were treated with Shikonin for 0-24 h, expression of indicated mitochondrial proteins were performed as described in Methods. Experiments were repeated minimum two-four times.

p-PERK / PERK / p-eIF2α / eIF2α / GRP78 / CHOP ; 

PubMed: 25879420     


Shikonin treatment induces ER stress associated protein expression. Western blot experiments in prostate cancer cells treated with 2.5 μM of Shikonin increased the phosphorylation of PERK, and its substrate eIF2α, increased expression of GRP78/Bip and CHOP/GADD135 in a time-dependent manner.

MMP-2 / MMP-9 ; 

PubMed: 26473829     


Shikonin inhibited the expression and activity of MMP-2 and MMP-9. U87 and U251 cells were treated with shikonin at 2.5, 5, and 7.5 μmol/L for 48 h. Serum free DMEM served as a negative control. Expressions of MMP-2 and MMP-9 were checked with Western Blot. (A) Effects of shikonin on the expression of MMP-2 in U87 cells; (B) Effects of shikonin on the expression of MMP-9 in U87 cells; (C) The changing pattern of MMP-2 in U251 cells; (D) The changing pattern of MMP-9 in U251 cells; (E) Effects of shikonin on the activities of MMP-2 and MMP-9 in U87 cells; (F) Effects of shikonin on the activities of MMP-2 and MMP-9 in U251 cells. Statistical analysis showed that shikonin significantly reduced the expression levels and activity of both MMP-2 and MMP-9 proteins compared with the control group in a dose-dependent manner. * p < 0.05, ** p < 0.01 (compared with control group); # p < 0.05 (compared with 2.5 μmol/L groups) (n = 5).

p-β-catenin / β-catenin ; 

PubMed: 26473829     


(A) Western blot assay results of β-catenin and p-β-catenin Y333 in U87 cells. (D) Western blot assay results of β-catenin and p-β-catenin Ser45 in U87 cells.

25879420 26473829
Growth inhibition assay
Cell viability; 

PubMed: 25879420     


Shikonin treatment inhibits prostate cancer cell viability without affecting normal prostate epithelial cells. DU-145, PC-3 and PrEC cells were treated with various doses (0.5, 1, 2.5, 5 and 10 μM) of Shikonin for 24 h and CCK-8 assay was used for the measurement of cell viability.

25879420
体内試験

Shikonin significantly delays intestinal motility in mice and reduces stool water content in a neonatal mice model of rotaviral diarrhea without affecting the viral infection process in vivo. Shikonin has been reported to have antioxidant, antibacterial, antiparasitic, antiviral and wound-healing activities. Shikonin inhibits allergic action as well as tracheal hyperresponsiveness in vivo. Intraperitonal injection of shikonin has been demonstrated to result in some toxicity, with an LD50 of 20 mg/kg. Shikonin absorption is fast if given by oral gavage and muscle injection, as it is barely detected in the plasma after 1 min, with a oral gavage yielding a bioavailability of about 34%[2].

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

- 合併
  • 細胞株: Human monocytes
  • 濃度: 10, 1, 0.1, 0.01 μM
  • 反応時間: 12 and 24 hours
  • 実験の流れ:

    Freshly isolated human monocytes are plated in a 96-microwell plate (Costar) at 105 cells per well with shikonin at a final concentration of 10, 1, 0.1, 0.01 μM. The numbers of viable cells, as detected by MTS test and the trypan blue exclusion assay, were measured 12 and 24 h after incubation at 37°C in humidified air with 5% CO2.


    (参考用のみ)
動物試験:

[2]

- 合併
  • 動物モデル: Neonatal ICR mice
  • 投薬量: 0.4 and 1.7 μg in 30 μL PBS
  • 投与方法: oral administration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 57 mg/mL (197.71 mM)
Ethanol 23 mg/mL (79.77 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
混合させたのち直ちに使用することを推奨します。
0.23mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 288.30
化学式

C16H16O5

CAS No. 54952-43-1
Storage powder
in solvent
別名 Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844
Smiles CC(=CCC(C1=CC(=O)C2=C(C=CC(=C2C1=O)O)O)O)C

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

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