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 16900
JPY 30200
JPY 96600
JPY 163000
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文献中Selleckの製品使用例(103)

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 MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIr1XmFKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUiyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF4IH7NMi=> MV3TRW5ITVJ?
human GCT cell M4C3cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{nkNmlvcGmkaYTpc44hd2ZiaIXtZY4hT0OWIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{C2MlczKG6PLh?= NUDGR2RTW0GQR1XS
human 769-P cell M3vxeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3KfIIyUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> MlflV2FPT0WU
human LOXIMVI cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmriTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> MmPZV2FPT0WU
human D-336MG cell NFjJSIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OFYvOiCwTT6= NG\TVWJUSU6JRWK=
human S-117 cell NWL4[HRJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWXJcohq[mm2aX;uJI9nKGi3bXHuJHMuOTF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKxMlMyKG6PLh?= MVvTRW5ITVJ?
human D-247MG cell NUnjbHFET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIrvRlNKdmirYnn0bY9vKG:oIHj1cYFvKERvMkS3UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PDhwNUKgcm0v M1vicHNCVkeHUh?=
human TYK-nu cell NYjDRmlsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH:3VFNKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODd7IN88UU4> Mnj3V2FPT0WU
human A498 cell NWrqN4VuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV3MWI1pUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{KM7:TT6= MUfTRW5ITVJ?
human HepG2 cells NUHyeI41TnWwY4Tpc44h[XO|YYm= NIHR[|U{KGh? NH6zfmpKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG3ncJVkd3OnIHnueI8h\2y7Y3;n[Y4h[W[2ZYKgN{BpenNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> MXuyNlI3OTB{Mx?=
human BCPAP cell M3rrd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJGJEWEGSIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62O{DPxE1w MWHTRW5ITVJ?
human KYSE-180 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnPxTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzNizszNMi=> M4PkfnNCVkeHUh?=
human MIA-PaCa-2 cell MojpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjaPI5YUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OkDPxE1w NHruT5pUSU6JRWK=
human HCC1395 cell NH7HcG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\YZVVDUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55ODFOwG0v M3rvRXNCVkeHUh?=
human RS4-11 cell NX3PTIVwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPVUh|ryPLh?= MYHTRW5ITVJ?
human NCI-H2122 cell MoD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjhizszNMi=> Moj1V2FPT0WU
human SNU-423 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHTxNpVKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNTFOwG0v M37sb3NCVkeHUh?=
human SK-LMS-1 cell NHr1To9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVvnS2lrUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwNkSg{txONg>? NYfw[JN5W0GQR1XS
human RPMI-7951 cell MnPiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvN{m1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F697zOIFnDOVA:Oi55IN88UU4> MUTTRW5ITVJ?
human COLO-829 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOEK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44PjV2IN88UU4> MnPCV2FPT0WU
human SCC-9 cell M1fTeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIG4T4tKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk46PSEQvF2u MVLTRW5ITVJ?
human A704 cell MmHqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrxTY5pcWKrdHnvckBw\iCqdX3hckBCPzB2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6wPFEzKM7:TT6= MVrTRW5ITVJ?
human HOP-62 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NITFVotKdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzZyNUSg{txONg>? Ml:3V2FPT0WU
human HCC1569 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlP0TY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNU[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDNyNTFOwG0v MnL5V2FPT0WU
human A172 cell MlKwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPzW5c1UW6qaXLpeIlwdiCxZjDoeY1idiCDMUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{44PTR7ODFOwG0v MV3TRW5ITVJ?
human MOLT-16 cell MlrpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg5PTV4IN88UU4> MYXTRW5ITVJ?
human TE-15 cell MlLiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HtUGlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2OzR|IN88UU4> Mo\FV2FPT0WU
human OE19 cell MkTUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJG9GOTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lkm2OFUyKM7:TT6= MlzFV2FPT0WU
human MHH-ES-1 cell M{X4NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1;SWWlvcGmkaYTpc44hd2ZiaIXtZY4hVUiKLVXTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB2NUS1JO69VS5? MoKyV2FPT0WU
human NKM-1 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\oXnpKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yOzl5MTFOwG0v MYHTRW5ITVJ?
human RCC10RGB cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKGi3bXHuJHJESzFyUlfCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4zQTR5OTFOwG0> NWHQZYNvW0GQR1XS
human BxPC-3 cell NVPmenA4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIDPPZBKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzB|OUGg{txONg>? M4fOSnNCVkeHUh?=
human ALL-PO cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWfyT4txUW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njh|OEW4JO69VS5? NG\1PJNUSU6JRWK=
human SK-OV-3 cell NYfrblB2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rR[2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTl|NDFOwG0v NYfSeoN5W0GQR1XS
human SW1710 cell MoPtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVjhfIZzUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? MYHTRW5ITVJ?

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

アッセイ
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

30709379 23993102 24165128
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3-30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
SOX10/EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

28174705 24779365
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