CHIR-99021 (CT99021) HCl

For research use only. Not for use in humans.

製品コードS2924

CHIR-99021 (CT99021) HCl化学構造

CAS No. 1797989-42-4

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

サイズ 価格(税別)  
JPY 30200
JPY 96600
JPY 148400
最寄りの販売代理店を探す

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バルク問合せ

文献中Selleckの製品使用例(388)

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) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
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] In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ). [2] Unlike lithium chloride and AR-A014418, CHIR-99021 treatment does not reduce the viability of INS-1E cells even at high concentrations. Instead, CHIR-99021 robustly increases the rate of proliferation of INS-1E cells in a dose-dependent manner, and significantly inhibits INS-E cell death induced by high glucose and high palmitate in a concentration-dependent manner. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 μM, with 2-3 fold increase of cell replication at 5 μM of CHIR-99021 treatment. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 NHfqXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPuN2JKSzVyPUmwNE4zOzFizszN Mlq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1155 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e3SmlEPTB;OEG4MlA2QSEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
BC-3 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzlSY9KSzVyPUiwOU4zODNizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KARPAS-422 NVvQSmE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX2cZFKSzVyPUe4PU4{OTVizszN NHPzWWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
DEL MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTdyMD64N|gh|ryP M{X0dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KM-H2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33MbGlEPTB;Nkm5MlA2QSEQvF2= Mn[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
U-87-MG NXO2cGl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;CSXhKSzVyPU[5OE42QDVizszN M3HYWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\yXndKSzVyPU[5NE4yPzJizszN MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-16 M3;YRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrrXXBKSzVyPU[4NE41PjJizszN NYXjdJpzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
TUR NEPWU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUK3[WExUUN3ME22O|EvOzJ{IN88US=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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NCI-H226 NHfvRYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTZT3J6UUN3ME22NlgvOzV|IN88US=> M2\TOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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KARPAS-45 NV7lSY9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7MW2FCUUN3ME22NVgvOjJzIN88US=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
ML-2 NU\G[m1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLrcnMxUUN3ME22NFYvPTd7IN88US=> MmHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
LP-1 NXfLb2IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK2PJRKSzVyPU[wN{42QDdizszN NEKzWXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
L-428 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;3TWM2OD14MECuOlcyKM7:TR?= NXX1R3N{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
K052 Mmi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TxOWlEPTB;NUe5MlIyOyEQvF2= Mn;kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
CAL-148 NUHJUJNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjRV5JKSzVyPUW2OU4xQDlizszN MnfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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EW-11 NYrpc5o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;jPHVKSzVyPUW1Nk4{QTlizszN NXLJNG5MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
COLO-320-HSR MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTV3MT6zOUDPxE1? NY\yOW5mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H889 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIX2[|NKSzVyPUW0O{4zOyEQvF2= NV\xVGJsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
EVSA-T NGPlc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTV2Mz62PFQh|ryP NGrZbW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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HSC-4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvyXlJNUUN3ME21N|kvOjl|IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H2227 M{XOcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fCOGlEPTB;NUOwMlI2PCEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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