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(税別) 在庫  
JPY 14940.00 あり
JPY 28220.00 あり
JPY 94620.00 あり
JPY 161020.00 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 NVf5NHRnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE3KG6PLh?= MWPTRW5ITVJ?
human GCT cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mli3TY5pcWKrdHnvckBw\iCqdX3hckBIS1RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ME[uO|Ihdk1w MWjTRW5ITVJ?
human 769-P cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLPUJRCUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> NIK0[GNUSU6JRWK=
human LOXIMVI cell M4nTT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1jWZmlvcGmkaYTpc44hd2ZiaIXtZY4hVE:[SV3WTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5QC5|MjDuUU4> NGf4UY9USU6JRWK=
human D-336MG cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjFTY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFQ3NjJibl2u MXzTRW5ITVJ?
human S-117 cell Mo\nS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= M3n0d3NCVkeHUh?=
human D-247MG cell M1nSS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4\ae2lvcGmkaYTpc44hd2ZiaIXtZY4hTC1{NEfNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1QC53MjDuUU4> NYG1OZZ1W0GQR1XS
human TYK-nu cell MmmxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXuxXlFwUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v NIXBZ4tUSU6JRWK=
human A498 cell NV7tbWxoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEDpVlZKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NFvRUlFUSU6JRWK=
human HepG2 cells NF\uNndHfW6ldHnvckBie3OjeR?= MoK2N{Bp MYXJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmOxcoDvdoF1cW:wIH;mJHs{UF2pbIXjc5NmKGmwdH:g[4x6[2:pZX6gZYZ1\XJiMzDodpMh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbne= NWTISG9XOjJ{NkGwNlM>
human BCPAP cell Mn3hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\PbW9IUW6qaXLpeIlwdiCxZjDoeY1idiCEQ2DBVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjdizszNMi=> NHTvXHZUSU6JRWK=
human KYSE-180 cell NWfuUHNbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH\3RllKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55MzFOwG0v NEHzcYxUSU6JRWK=
human MIA-PaCa-2 cell MmrwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\yTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55NjFOwG0v NVqzUlB1W0GQR1XS
human HCC1395 cell NIHWfY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIDsfXZKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{GzPVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjd6IN88UU4> MnrUV2FPT0WU
human RS4-11 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PneWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u MVPTRW5ITVJ?
human NCI-H2122 cell MnPFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XEWGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{ODFOwG0v MYrTRW5ITVJ?
human SNU-423 cell NGnKWXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;STY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0zNjVizszNMi=> M4XYPHNCVkeHUh?=
human SK-LMS-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3ux[GlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ2IN88UU4> NVrHNW5GW0GQR1XS
human RPMI-7951 cell M3vLRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3f1e2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XoxvJygTWM2OD1{Lkeg{txONg>? NGnncJBUSU6JRWK=
human COLO-829 cell Moe2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\yN|JKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi55NkW0JO69VS5? M4rnbnNCVkeHUh?=
human SCC-9 cell MoCxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPROYR{UW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTVizszNMi=> M13seXNCVkeHUh?=
human A704 cell M4LCV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7wWWtKdmirYnn0bY9vKG:oIHj1cYFvKEF5MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlA5OTJizszNMi=> NGHWSJRUSU6JRWK=
human HOP-62 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4HaUmlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v M334R3NCVkeHUh?=
human HCC1569 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF3NkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OzB3IN88UU4> NWTUZWdRW0GQR1XS
human A172 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mor6TY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63OVQ6QCEQvF2u MoDZV2FPT0WU
human MOLT-16 cell M4i5NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1jP[mlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDh3NU[g{txONg>? NX;KUYJmW0GQR1XS
human TE-15 cell NXzWbJBnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OVM1OyEQvF2u M3jFbXNCVkeHUh?=
human OE19 cell M4rJbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYPJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= MWXTRW5ITVJ?
human MHH-ES-1 cell MmjFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mmr3TY5pcWKrdHnvckBw\iCqdX3hckBOUEhvRWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODR3NEWg{txONg>? MXvTRW5ITVJ?
human NKM-1 cell NVTKNHJsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlPWTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVM6PzFizszNMi=> NGPCXZlUSU6JRWK=
human RCC10RGB cell Ml7hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;2T2dKdmirYnn0bY9vKG:oIHj1cYFvKFKFQ{GwVmdDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5{OUS3PUDPxE1? M3u3XXNCVkeHUh?=
human BxPC-3 cell NFm2UGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|A{QTFizszNMi=> MkPSV2FPT0WU
human ALL-PO cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPFM5PThizszNMi=> MWHTRW5ITVJ?
human SK-OV-3 cell Mn7PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1e4UGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NFvldldUSU6JRWK=
human SW1710 cell M3m4NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml\LTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQzPDV4IN88UU4> M{TROnNCVkeHUh?=

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
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