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)  
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)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 NEfnNYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWT6TI8{UW6qaXLpeIlwdiCxZjDoeY1idiCVV{m4NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC5zNjDuUU4> NETC[HJUSU6JRWK=
human GCT cell NXja[VRmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\PZVdKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwOk44OiCwTT6= NV3p[XBIW0GQR1XS
human 769-P cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX[zeHpFUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU5PC57OTDuUU4> NVnnd4x7W0GQR1XS
human LOXIMVI cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPiTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVg5NjN{IH7NMi=> M2jBXHNCVkeHUh?=
human D-336MG cell M3\rNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rzfWlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg1Pi5{IH7NMi=> MkXJV2FPT0WU
human S-117 cell MnHkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLwXZk5UW6qaXLpeIlwdiCxZjDoeY1idiCVLUGxO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzOS5|MTDuUU4> NXXz[5hsW0GQR1XS
human D-247MG cell NE\HSHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGQuOjR5TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OFgvPTJibl2u MYXTRW5ITVJ?
human TYK-nu cell MlfLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFc6KM7:TT6= Mnq0V2FPT0WU
human A498 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NID4UIFKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMh|ryPLh?= NXTuU4pOW0GQR1XS
human HepG2 cells MXHGeY5kfGmxbjDhd5NigQ>? M3TY[|MhcA>? M3nJWGlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXXfseYNwe2ViaX70c{BodHmlb3flckBi\nSncjCzJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> MVWyNlI3OTB{Mx?=
human BCPAP cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYC5XolQUW6qaXLpeIlwdiCxZjDoeY1idiCEQ2DBVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjdizszNMi=> NWjZVYhlW0GQR1XS
human KYSE-180 cell NF\6XoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44OyEQvF2u NXnZdJc4W0GQR1XS
human MIA-PaCa-2 cell NIHuRllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;pdJlKdmirYnn0bY9vKG:oIHj1cYFvKE2LQT3QZWNiNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLke2JO69VS5? M{DxbnNCVkeHUh?=
human HCC1395 cell MmTQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7UPIFMUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxN|k2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS55ODFOwG0v M2HJeHNCVkeHUh?=
human RS4-11 cell M2fseGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vxSWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46PSEQvF2u MmTDV2FPT0WU
human NCI-H2122 cell NUTWUWl4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkGyNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjhizszNMi=> NIXTUJdUSU6JRWK=
human SNU-423 cell MkDZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLLc|hKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNTFOwG0v MWXTRW5ITVJ?
human SK-LMS-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF65Z5ZKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi54NDFOwG0v M17WVnNCVkeHUh?=
human RPMI-7951 cell NUfwXYRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnvKTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTJwNzFOwG0v MU\TRW5ITVJ?
human COLO-829 cell Ml\OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHSTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUiyPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPzZ3NDFOwG0v MX7TRW5ITVJ?
human SCC-9 cell M{LjZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4nUemlvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlk2KM7:TT6= MXrTRW5ITVJ?
human A704 cell NV\t[otvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\mTY5pcWKrdHnvckBw\iCqdX3hckBCPzB2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6wPFEzKM7:TT6= NVK0SWRFW0GQR1XS
human HOP-62 cell M1L0OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{TpeGlvcGmkaYTpc44hd2ZiaIXtZY4hUE:SLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{PjB3NDFOwG0v NYSyenMxW0GQR1XS
human HCC1569 cell Mo\tS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NITGNIZKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G1Olkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjR6M{C1JO69VS5? NF75c2tUSU6JRWK=
human A172 cell MoD5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{fwd2lvcGmkaYTpc44hd2ZiaIXtZY4hSTF5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|U1QThizszNMi=> NIryRnVUSU6JRWK=
human MOLT-16 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIHPeINKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh6NUW2JO69VS5? MlzQV2FPT0WU
human TE-15 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmXPTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVU{PDNizszNMi=> MnL2V2FPT0WU
human OE19 cell NIG2UXVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEO1[HdKdmirYnn0bY9vKG:oIHj1cYFvKE:HMUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk3PDVzIN88UU4> MVzTRW5ITVJ?
human MHH-ES-1 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG1JUC2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xPDV2NTFOwG0v MWLTRW5ITVJ?
human NKM-1 cell NGqxOpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnZT3ZrUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTN7N{Gg{txONg>? NV\hXo9CW0GQR1XS
human RCC10RGB cell M1PQO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJHJESzFyUlfCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4zQTR5OTFOwG0> NWDPS3NlW0GQR1XS
human BxPC-3 cell NVPJWXM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|A{QTFizszNMi=> MmnkV2FPT0WU
human ALL-PO cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13nN2lvcGmkaYTpc44hd2ZiaIXtZY4hSUyOLWDPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE45Ozh3ODFOwG0v NV[4fplFW0GQR1XS
human SK-OV-3 cell M1Tobmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk6OzRizszNMi=> NWLDW2ozW0GQR1XS
human SW1710 cell MljZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUfTWIZ7UW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjR{NEW2JO69VS5? NIO0O|lUSU6JRWK=

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

Related Antibodies

GSK-3信号経路図

GSK-3 Inhibitors with Unique Features

相関GSK-3製品

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
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID