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(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) 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 NFK4VGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnyOZRSUW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> M2n0Z3NCVkeHUh?=
human GCT cell NVnmNGlPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mle1TY5pcWKrdHnvckBw\iCqdX3hckBIS1RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ME[uO|Ihdk1w NGjQfWVUSU6JRWK=
human 769-P cell MknwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVTJcohq[mm2aX;uJI9nKGi3bXHuJFc3QS2SIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUi0Mlk6KG6PLh?= NUTNXlUyW0GQR1XS
human LOXIMVI cell M4\DcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjBbpBzUW6qaXLpeIlwdiCxZjDoeY1idiCOT2jJUXZKKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PTh6LkOyJI5ONg>? MoTiV2FPT0WU
human D-336MG cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGDEdlVKdmirYnn0bY9vKG:oIHj1cYFvKERvM{O2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PDZwMjDuUU4> MmH5V2FPT0WU
human S-117 cell NE[5SoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYXIRnE2UW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> MnS0V2FPT0WU
human D-247MG cell NHnPd4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUiybVljUW6qaXLpeIlwdiCxZjDoeY1idiCGLUK0O21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTR6LkWyJI5ONg>? M1rRV3NCVkeHUh?=
human TYK-nu cell Mmn2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnsPYVCUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5OTFOwG0v MV7TRW5ITVJ?
human A498 cell NYrvR2RbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkTKTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zJO69VS5? NWrTXFdlW0GQR1XS
human HepG2 cells NHPqZ4FHfW6ldHnvckBie3OjeR?= MmW1N{Bp NWfRdWFYUW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jd[4x2[2:|ZTDpcpRwKGeueXPv[4VvKGGodHXyJFMhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o MXGyNlI3OTB{Mx?=
human BCPAP cell NHPKO3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XnfWlvcGmkaYTpc44hd2ZiaIXtZY4hSkOSQWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY4KM7:TT6= MkPkV2FPT0WU
human KYSE-180 cell NFH1XnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHf3UlVKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55MzFOwG0v MVnTRW5ITVJ?
human MIA-PaCa-2 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\Mb2tKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? NIPnO|lUSU6JRWK=
human HCC1395 cell NXr3[mV3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGhESzF|OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc5KM7:TT6= MWLTRW5ITVJ?
human RS4-11 cell NH\UfYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnv1TY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2KM7:TT6= NVr4cnh4W0GQR1XS
human NCI-H2122 cell NXfafFNoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWPUUWNXUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4JO69VS5? NXjKcI1HW0GQR1XS
human SNU-423 cell NYHqXXB[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEH5NIRKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNTFOwG0v NUPEboVDW0GQR1XS
human SK-LMS-1 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Moq2TY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjRizszNMi=> M1Tld3NCVkeHUh?=
human RPMI-7951 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGe0WnhKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G778{MJGlEPTB;Mj63JO69VS5? NWTxUnRoW0GQR1XS
human COLO-829 cell NXXMXoFVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOEK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44PjV2IN88UU4> NEj3U3NUSU6JRWK=
human SCC-9 cell MoDPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGi3bXHuJHNESy17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj65OUDPxE1w M4K3W3NCVkeHUh?=
human A704 cell MlHyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mmm5TY5pcWKrdHnvckBw\iCqdX3hckBCPzB2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6wPFEzKM7:TT6= MX7TRW5ITVJ?
human HOP-62 cell M3zDO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{CzT2lvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v MmHUV2FPT0WU
human HCC1569 cell M1vpUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfhTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNU[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDNyNTFOwG0v NG\E[IpUSU6JRWK=
human A172 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjUTY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63OVQ6QCEQvF2u NF;jUllUSU6JRWK=
human MOLT-16 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHTMN2ZKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh6NUW2JO69VS5? MYHTRW5ITVJ?
human TE-15 cell NVf1S3BmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHzBdVZKdmirYnn0bY9vKG:oIHj1cYFvKFSHLUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PTN2MzFOwG0v M1y4fXNCVkeHUh?=
human OE19 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= NG\B[XZUSU6JRWK=
human MHH-ES-1 cell NWPrTlBtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrncoxKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yNEW0OUDPxE1w MV;TRW5ITVJ?
human NKM-1 cell NH[3[4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUH5TIN[UW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTN7N{Gg{txONg>? MljRV2FPT0WU
human RCC10RGB cell NU\xb2ExT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmDuTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOjl2N{mg{txO M2TabXNCVkeHUh?=
human BxPC-3 cell NF3DeGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\mZmlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44ODN7MTFOwG0v NFzPcJVUSU6JRWK=
human ALL-PO cell M4rhS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmrDTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlg{QDV6IN88UU4> MY\TRW5ITVJ?
human SK-OV-3 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnK0TY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46QTN2IN88UU4> Mo[wV2FPT0WU
human SW1710 cell NIm5fWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXwbmJKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDJ2NU[g{txONg>? MWDTRW5ITVJ?

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 左から右までの手順で、溶剤を製品に加えることです:
4% DMSO+30% PEG 300+ddH2O
いい結果が出るために、混じった後、直ちに使うと推めます。
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

Related Antibodies

GSK-3シグナル伝達経路

GSK-3 Inhibitors with Unique Features

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Tags: CHIR-99021 (CT99021)を買う | CHIR-99021 (CT99021) ic50 | CHIR-99021 (CT99021)供給者 | CHIR-99021 (CT99021)を購入する | CHIR-99021 (CT99021)費用 | CHIR-99021 (CT99021)生産者 | オーダーCHIR-99021 (CT99021) | CHIR-99021 (CT99021)化学構造 | CHIR-99021 (CT99021)分子量 | CHIR-99021 (CT99021)代理店
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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