CHIR-99021 (CT99021) HCl

For research use only. Not for use in humans.

目录号:S2924

CHIR-99021 (CT99021) HCl Chemical Structure

CAS No. 1797989-42-4

CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂,IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy,并可增强 GR,RORα和自噬相关蛋白等表达。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2780.99 现货
RMB 733.53 现货
RMB 1373.92 现货
RMB 4650.09 现货
RMB 8330.15 现货
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客户使用Selleck生产的CHIR-99021 (CT99021) HCl发表文献320篇:

产品安全说明书

GSK-3抑制剂选择性比较

生物活性

产品描述 CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂,IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy,并可增强 GR,RORα和自噬相关蛋白等表达。
靶点
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
体外研究

CHIR-99021作用于GSK-3比作用于其最接近的同系物CDC2和ERK2,及其他蛋白激酶选择性高500倍。此外,CHIR-99021只与一组22种药理相关的受体微弱结合,且对一组23种非激酶的酶几乎没有抑制活性。CHIR-99021作用于表达胰岛素受体的CHO-IR细胞,诱导糖原合成酶(GS)激活,EC50为0.763 μM。[1]CHIR-99021(3 μM)作用于3T3-L1前脂肪细胞,除了模拟胰岛素的作用,抑制GSK-3,使胞内游离β-catenin增加1.9倍,模仿经典Wnt信号通路。在分化的前3天,CHIR-99021处理,抑制脂肪细胞分化,IC50为0.3 μM,通过抑制CCAAT/增强子结合蛋白α(C/EBPα)和过氧化物酶体增殖物激活受体γ(PPARγ)的诱导作用。[2] 不像LiCl和AR-A014418,CHIR-99021处理,即使在高浓度,不会降低INS-1E细胞活力。相反,CHIR-99021增加INS-1E细胞增殖,这种作用具有剂量依赖性,且显著抑制高糖和高棕榈酸诱导的INS-E细胞死亡,这种作用具有浓度依赖性。CHIR-99021浓度低至1 μM,处理离体大鼠胰岛,促进β细胞复制,5 μM CHIR-99021处理,使细胞复制增长2-3倍。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 M16xRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLvb|J1UUN3ME25NFAvOjNzIN88US=> NEPGeGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H1155 M3u5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moi3TWM2OD16MUiuNFU6KM7:TR?= NGrBNFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
BC-3 NF\rbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRThyNT6yNFMh|ryP NYfSNHVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
KARPAS-422 NF71VVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTd6OT6zNVUh|ryP MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
DEL MnT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTVTWM2OD15MECuPFM5KM7:TR?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KM-H2 NIPxXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXtZW1FUUN3ME22PVkvODV7IN88US=> NEThR5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
U-87-MG NVvkXmZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7zcGRsUUN3ME22PVQvPTh3IN88US=> M3zjeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-1 M4fDcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHWTWM2OD14OUCuNVczKM7:TR?= M1W1SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-16 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHUTWM2OD14OECuOFYzKM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
TUR NHnObGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFWzdZNKSzVyPU[3NU4{OjJizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
IM-9 M4HXTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTZ3MT61OFEh|ryP MmG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
L-363 M3HQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3vTWM2OD14NEiuNFY1KM7:TR?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H226 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnuZ2pKSzVyPU[yPE4{PTNizszN NGizSFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HT M4n3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrpflRKSzVyPU[yNk44QDVizszN M{jRU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KARPAS-45 NV3PdWxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzn[mRuUUN3ME22NVgvOjJzIN88US=> NEOxb4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
ML-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPLTWM2OD14ME[uOVc6KM7:TR?= NHTLNmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
LP-1 MorwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\hTWM2OD14MEOuOVg4KM7:TR?= NIfsVHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
L-428 NHjBTXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fsTmlEPTB;NkCwMlY4OSEQvF2= MoT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
K052 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv5WZpKSzVyPUW3PU4zOTNizszN MnP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
CAL-148 NH7hO3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnoTWM2OD13NkWuNFg6KM7:TR?= NV;rdXpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
UACC-812 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;sZ3NzUUN3ME21OVkvOzlzIN88US=> Mln5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
EW-11 M{jMTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrjTWM2OD13NUKuN|k6KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
COLO-320-HSR Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXxTWM2OD13NUGuN|Uh|ryP Mn3xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H889 NX7U[nprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4W1V2lEPTB;NUS3MlI{KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
EVSA-T NHXvOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjGSlQyUUN3ME21OFMvPjh2IN88US=> NFvjRlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
RL M4LxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS3V2xxUUN3ME21OFIvPDR{IN88US=> NHP5PY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HSC-4 M{LlZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTV|OT6yPVMh|ryP NGOwbnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H2227 NWnqV3ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fE[2lEPTB;NUOwMlI2PCEQvF2= M2LNSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NB5 NUXMWmVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzPTWM2OD13Mk[uOFMh|ryP NELZRlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H2081 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3k[|BKSzVyPUWyOU42OTNizszN NFS1cYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H510A NVTBfZpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV21OYQ2UUN3ME21NlQvPjl4IN88US=> MoCxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1436 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[3WmRKSzVyPUWyN{4xPjRizszN NFW1NXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HL-60 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFviZnpKSzVyPUWyNk46OjRizszN Mke5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
Mo-T MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILTRWpKSzVyPUWxOU4yOTZizszN NV22eVU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H2171 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jibWlEPTB;NUGyMlcxPSEQvF2= NWjPXlZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H1694 MnzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLjfYJjUUN3ME21NVIvPDN7IN88US=> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
P12-ICHIKAWA MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnvbpZuUUN3ME21NVEvPDF4IN88US=> NWDhUlNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
DU-4475 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfNToVWUUN3ME21NVEvOTBzIN88US=> MlPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
RPMI-8402 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTVzMD6wNlEh|ryP NWDMOphkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
EHEB MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVyNz6yNFgh|ryP NGj6bpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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