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 M{TSWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEmzTpNKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> NI\NUFFUSU6JRWK=
human GCT cell MkHnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXL0S2JQUW6qaXLpeIlwdiCxZjDoeY1idiCJQ2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFYvPzJibl2u M2LEe3NCVkeHUh?=
human 769-P cell NHG4Z5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jMe2lvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFQvQTlibl2u NVzPN2RvW0GQR1XS
human LOXIMVI cell M4DIUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3HfHJKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QDhwM{Kgcm0v MW\TRW5ITVJ?
human D-336MG cell NGXhWoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;nTY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFQ3NjJibl2u MkjJV2FPT0WU
human S-117 cell NUDVXVJVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4foU2lvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25NlEvOzFibl2u NITENZVUSU6JRWK=
human D-247MG cell M1LXcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7uTY5pcWKrdHnvckBw\iCqdX3hckBFNTJ2N13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQ5NjV{IH7NMi=> MVHTRW5ITVJ?
human TYK-nu cell NFP0TnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGn2d29KdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODd7IN88UU4> M4fycXNCVkeHUh?=
human A498 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWjJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOg{txONg>? M3fLfXNCVkeHUh?=
human HepG2 cells M4\WTGZ2dmO2aX;uJIF{e2G7 MlH5N{Bp MXvJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmOxcoDvdoF1cW:wIH;mJHs{UF2pbIXjc5NmKGmwdH:g[4x6[2:pZX6gZYZ1\XJiMzDodpMh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbne= NHLjSmIzOjJ4MUCyNy=>
human BCPAP cell NWjvUGRpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml[2TY5pcWKrdHnvckBw\iCqdX3hckBDS1CDUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlch|ryPLh?= Mm[5V2FPT0WU
human KYSE-180 cell NY\2fGNmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnzRTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> NWDuSolwW0GQR1XS
human MIA-PaCa-2 cell NEPiVYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXOwZVd1UW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OkDPxE1w NXPLcoRvW0GQR1XS
human HCC1395 cell M2HNemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfoTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzM{m1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44QCEQvF2u MV;TRW5ITVJ?
human RS4-11 cell M4jQbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUh|ryPLh?= NI[4RXlUSU6JRWK=
human NCI-H2122 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjhizszNMi=> MmHUV2FPT0WU
human SNU-423 cell MkjNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zR[mlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUSyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi53IN88UU4> M1zhPHNCVkeHUh?=
human SK-LMS-1 cell M2\qWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1vSe2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTF3TMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ2IN88UU4> MX\TRW5ITVJ?
human RPMI-7951 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvN{m1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi55IN88UU4> M{P4OHNCVkeHUh?=
human COLO-829 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHrRWhlUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwN{[1OEDPxE1w NW\wS5NUW0GQR1XS
human SCC-9 cell MmrsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoTXTY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= Mon3V2FPT0WU
human A704 cell NFHafGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XwW2lvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFgyOiEQvF2u Mn:2V2FPT0WU
human HOP-62 cell NYj0[IpwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NILmcmxKdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzZyNUSg{txONg>? Ml;MV2FPT0WU
human HCC1569 cell MnW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\QSWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUW2PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDh|MEWg{txONg>? M3;XS3NCVkeHUh?=
human A172 cell MlS2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPCUodzUW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{44PTR7ODFOwG0v MYLTRW5ITVJ?
human MOLT-16 cell NVPVNFIyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVfQ[JRIUW6qaXLpeIlwdiCxZjDoeY1idiCPT1zUMVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy56OEW1OkDPxE1w MWfTRW5ITVJ?
human TE-15 cell M{ez[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PIfGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> MkfzV2FPT0WU
human OE19 cell NFfoW4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{nSRWlvcGmkaYTpc44hd2ZiaIXtZY4hV0VzOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVY1PTFizszNMi=> NIfFVHhUSU6JRWK=
human MHH-ES-1 cell NXXSWYg5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYHiPVk6UW6qaXLpeIlwdiCxZjDoeY1idiCPSFitSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMES1OFUh|ryPLh?= M3X1e3NCVkeHUh?=
human NKM-1 cell NHnzb41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnFTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuNVM6PzFizszNMi=> NXPpWWVbW0GQR1XS
human RCC10RGB cell M{n3VWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3;HWmlvcGmkaYTpc44hd2ZiaIXtZY4hWkOFMUDSS2Ih[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjJ7NEe5JO69VQ>? Mn2yV2FPT0WU
human BxPC-3 cell NXvGToc3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|A{QTFizszNMi=> M3r0U3NCVkeHUh?=
human ALL-PO cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2LLUmlvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45Ozh3ODFOwG0v MmXLV2FPT0WU
human SK-OV-3 cell NGnQNG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk6OzRizszNMi=> MWDTRW5ITVJ?
human SW1710 cell Ml7MS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{KwTGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41OjR3NjFOwG0v M1GxfXNCVkeHUh?=

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