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) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

サイズ 価格(税別)  
JPY 14940.00
JPY 28220.00
JPY 94620.00
JPY 161020.00

カスタマーフィードバック(2)

  • Lu1205 were treated with protein kinase inhibitors. Cell cycle protein expression was analyzed by western blot.

    Med Oncol, 2017, 35(1):7. CHIR-99021 (CT99021) purchased from Selleck.

    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) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.
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 NF7UW3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE3KG6PLh?= NVzCNYZjW0GQR1XS
human GCT cell NFnNcWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGdEXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNyNj63NkBvVS5? MU\TRW5ITVJ?
human 769-P cell NF\rRnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJFc3QS2SIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUi0Mlk6KG6PLh?= M3\pPHNCVkeHUh?=
human LOXIMVI cell MlH6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJGxQYEmPVlmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21PFgvOzJibl2u NHTaTWFUSU6JRWK=
human D-336MG cell NEez[3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OFYvOiCwTT6= Ml7wV2FPT0WU
human S-117 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TEd2lvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25NlEvOzFibl2u NV;TWIpyW0GQR1XS
human D-247MG cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJGQuOjR5TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OFgvPTJibl2u MXrTRW5ITVJ?
human TYK-nu cell M1rrNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fDWmlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPzlizszNMi=> M{PUPXNCVkeHUh?=
human A498 cell M{PtbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVPJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOg{txONg>? MWPTRW5ITVJ?
human HepG2 cells MWDGeY5kfGmxbjDhd5NigQ>? MnnaN{Bp NH\IPIdKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> M3HpNVIzOjZzMEKz
human BCPAP cell MmX2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w M13BeXNCVkeHUh?=
human KYSE-180 cell Mn3DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHGUFVRUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVE5OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{Og{txONg>? M{TjXHNCVkeHUh?=
human MIA-PaCa-2 cell NHjqPFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlHUTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55NjFOwG0v NHz5fWFUSU6JRWK=
human HCC1395 cell MnfRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYH0Oo1yUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55ODFOwG0v NF3veGpUSU6JRWK=
human RS4-11 cell NYexNZhyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXnJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUh|ryPLh?= MVnTRW5ITVJ?
human NCI-H2122 cell MlXQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2S0NWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{ODFOwG0v NU\OdWNGW0GQR1XS
human SNU-423 cell NIrxN|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojGTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0zNjVizszNMi=> MUTTRW5ITVJ?
human SK-LMS-1 cell MlXGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEHIVohKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi54NDFOwG0v MXXTRW5ITVJ?
human RPMI-7951 cell M4rIfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrpUIFKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? NFHST4xUSU6JRWK=
human COLO-829 cell M{njN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHpTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUiyPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPzZ3NDFOwG0v MX\TRW5ITVJ?
human SCC-9 cell NV;ZbpVJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;ITY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPVUh|ryPLh?= MnzHV2FPT0WU
human A704 cell Mmm2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVIh|ryPLh?= MV;TRW5ITVJ?
human HOP-62 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELvbIFKdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzZyNUSg{txONg>? M3\oTnNCVkeHUh?=
human HCC1569 cell NHHCZmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW[weFhmUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOVY6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy52OEOwOUDPxE1w NUPHU2M6W0GQR1XS
human A172 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGe3XHFKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc2PDl6IN88UU4> MVrTRW5ITVJ?
human MOLT-16 cell M3fFSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn75TY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45QDV3NjFOwG0v MXPTRW5ITVJ?
human TE-15 cell M1W3d2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1TIc2lvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> MUfTRW5ITVJ?
human OE19 cell M2\ncmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVf5SFhLUW6qaXLpeIlwdiCxZjDoeY1idiCRRUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PjR3MTFOwG0v NGjodYlUSU6JRWK=
human MHH-ES-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xPDV2NTFOwG0v NGjLflFUSU6JRWK=
human NKM-1 cell NXGxS3B3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLwWJJWUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTN7N{Gg{txONg>? MmDVV2FPT0WU
human RCC10RGB cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4D0dWlvcGmkaYTpc44hd2ZiaIXtZY4hWkOFMUDSS2Ih[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjJ7NEe5JO69VQ>? M{nQXnNCVkeHUh?=
human BxPC-3 cell NV;yN|F4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXWVGhmUW6qaXLpeIlwdiCxZjDoeY1idiCEeGDDMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjdyM{mxJO69VS5? MojVV2FPT0WU
human ALL-PO cell MnPJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\KXZh{UW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njh|OEW4JO69VS5? MWHTRW5ITVJ?
human SK-OV-3 cell M3jHNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\1VWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NV3YcXdLW0GQR1XS
human SW1710 cell M1XNZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvQTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQzPDV4IN88UU4> NHu0NoRUSU6JRWK=

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

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 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):
4% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
3.5mg/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 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

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) 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

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

GSK-3シグナル伝達経路

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