CHIR-99021 (CT99021)

製品コードS1263

CHIR-99021 (CT99021)化学構造

分子量(MW):465.34

CHIR-99021 (CT99021)は一種のGSK-3αとGSK-3β阻害剤で、IC50値が10 nM と6.7 nMに分かれます。

サイズ 価格 在庫  
JPY 12958.92 あり
JPY 24477.96 あり
JPY 82073.16 あり
JPY 139668.35 あり

カスタマーフィードバック(1)

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells. 

    Dr. Yong-Weon Yi from Georgetown University Medical Center. CHIR-99021 (CT99021) purchased from Selleck.

製品安全説明書

GSK-3阻害剤の選択性比較

生物活性

製品説明 CHIR-99021 (CT99021)は一種のGSK-3αとGSK-3β阻害剤で、IC50値が10 nM と6.7 nMに分かれます。
ターゲット
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
体外試験

CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM[1].

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SW982 cell MoT0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4DEXmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvOTZibl2u NIPSd5hUSU6JRWK=
human GCT cell NWPyepZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHX6OFBKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= M2XmOHNCVkeHUh?=
human 769-P cell MojsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILMeXpKdmirYnn0bY9vKG:oIHj1cYFvKDd4OT3QJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg1Njl7IH7NMi=> M4\nZ3NCVkeHUh?=
human LOXIMVI cell NXnKcXhST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HHRmlvcGmkaYTpc44hd2ZiaIXtZY4hVE:[SV3WTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5QC5|MjDuUU4> NYjxUmhsW0GQR1XS
human D-336MG cell M{PuZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXzZpZKdmirYnn0bY9vKG:oIHj1cYFvKERvM{O2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PDZwMjDuUU4> NV\ReXpQW0GQR1XS
human S-117 cell NXTQdFlUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= MnTxV2FPT0WU
human D-247MG cell NHzTeG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTsTY5pcWKrdHnvckBw\iCqdX3hckBFNTJ2N13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQ5NjV{IH7NMi=> M1ixeXNCVkeHUh?=
human TYK-nu cell NYnxbIprT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXBNYJPUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v NFzVNm5USU6JRWK=
human A498 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXiTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zJO69VS5? NVvNd45wW0GQR1XS
human HepG2 cells NVzIXm91TnWwY4Tpc44h[XO|YYm= NYW4[2Z5OyCq NWPmcJRFUW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jd[4x2[2:|ZTDpcpRwKGeueXPv[4VvKGGodHXyJFMhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o Mn7zNlIzPjFyMkO=
human BCPAP cell MlLzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w M{TiNnNCVkeHUh?=
human KYSE-180 cell NX[w[Ih[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXLJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44OyEQvF2u NFrxdZNUSU6JRWK=
human MIA-PaCa-2 cell MnzuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd4IN88UU4> NGrUd4JUSU6JRWK=
human HCC1395 cell MlXDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4rmRmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUO5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzhizszNMi=> M4Gw[3NCVkeHUh?=
human RS4-11 cell NIHyUI5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4LUV2lvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u NUHLbFRoW0GQR1XS
human NCI-H2122 cell NYTUNHJHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXPCWZVJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? MnLLV2FPT0WU
human SNU-423 cell NYiyTFg2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXqyUFkzUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{LkWg{txONg>? NYTpUYl1W0GQR1XS
human SK-LMS-1 cell NFK3fY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLvWJNKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi54NDFOwG0v NH;FOYRUSU6JRWK=
human RPMI-7951 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvN{m1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi55IN88UU4> NUPneIV[W0GQR1XS
human COLO-829 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYDpOFRrUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w MWTTRW5ITVJ?
human SCC-9 cell M1vxdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJHNESy17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65OUDPxE1w MYDTRW5ITVJ?
human A704 cell M2fNXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUnNWVJZUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xQDF{IN88UU4> MlHSV2FPT0WU
human HOP-62 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|YxPTRizszNMi=> M3HXfHNCVkeHUh?=
human HCC1569 cell M1PpTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGXj[5JKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G1Olkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjR6M{C1JO69VS5? Mmf0V2FPT0WU
human A172 cell MlzNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1j6WGlvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> MVnTRW5ITVJ?
human MOLT-16 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHkTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45QDV3NjFOwG0v M3j4fnNCVkeHUh?=
human TE-15 cell NWjDXmo{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OVM1OyEQvF2u NF7YeWlUSU6JRWK=
human OE19 cell MnuyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIHJdWVKdmirYnn0bY9vKG:oIHj1cYFvKE:HMUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk3PDVzIN88UU4> M3[4R3NCVkeHUh?=
human MHH-ES-1 cell NXPJUYloT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvYeohPUW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= Mn;QV2FPT0WU
human NKM-1 cell NWnINZlVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7QfGhoUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTN7N{Gg{txONg>? NUHYVXdIW0GQR1XS
human RCC10RGB cell NHvUNGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvsTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO Mlz6V2FPT0WU
human BxPC-3 cell Ml2xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYThS|dDUW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? NEHHS2VUSU6JRWK=
human ALL-PO cell M3n0Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWThfnRYUW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njh|OEW4JO69VS5? NUi5[2FzW0GQR1XS
human SK-OV-3 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWjJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk6OzRizszNMi=> MULTRW5ITVJ?
human SW1710 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHFTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQzPDV4IN88UU4> MUjTRW5ITVJ?

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge[1].

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

+ 展開
  • 細胞株: Insulin receptor–expressing CHO-IR cells; Primary rat hepatocytes
  • 濃度: 0.01-10 μM
  • 反応時間: 30 min
  • 実験の流れ:

    CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 ml of medium without fetal bovine serum. After 24 h, medium is replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37°C. Cells are lysed and centrifuged 15 min at 4°C/14000g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mmol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Female db/db mice; Male ZDF rats
  • 製剤: HCl salts formulated
  • 投薬量: 8-48 mg/kg
  • 投与方法: oral administration
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 10 mg/mL (21.48 mM) warming
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+30% PEG 300+ddH2O
3.5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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 465.34
化学式

C22H18Cl2N8

CAS No. 252917-06-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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MSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

GSK-3信号経路図

GSK-3 Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID