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 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374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 NUSwO2R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTlyMD6yN|Eh|ryP MojZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1155 NVLQV|BVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XsdGlEPTB;OEG4MlA2QSEQvF2= MlHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
BC-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF24NHhKSzVyPUiwOU4zODNizszN M1;PO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KARPAS-422 NIGxPFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHDTIVCUUN3ME23PFkvOzF3IN88US=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
DEL NFnYVmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj5TWM2OD15MECuPFM5KM7:TR?= M{HqNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KM-H2 NIrGVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7pWIxKSzVyPU[5PU4xPTlizszN MoHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
U-87-MG NHfWb4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLqfHhzUUN3ME22PVQvPTh3IN88US=> M3fzPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-1 NGfzfYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjESm15UUN3ME22PVAvOTd{IN88US=> M3XwTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-16 M3vwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17sW2lEPTB;NkiwMlQ3OiEQvF2= NED0dlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
TUR MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW4SWJKSzVyPU[3NU4{OjJizszN NWTzSoJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
IM-9 M1XqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDqOmt[UUN3ME22OVEvPTRzIN88US=> M{X3fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
L-363 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W0OWlEPTB;NkS4MlA3PCEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H226 NWrUPZYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HtUGlEPTB;NkK4MlM2OyEQvF2= NXvaeogyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HT NIPqR5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17ER2lEPTB;NkKyMlc5PSEQvF2= NHq0cnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
KARPAS-45 NF7EdmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLFUIY6UUN3ME22NVgvOjJzIN88US=> M4rVelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
ML-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTRR3VJUUN3ME22NFYvPTd7IN88US=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
LP-1 NHvIXGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\WNmlEPTB;NkCzMlU5PyEQvF2= NVfJWnI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
L-428 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rNVWlEPTB;NkCwMlY4OSEQvF2= MnzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
K052 NUjsWJRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrSSIdSUUN3ME21O|kvOjF|IN88US=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
CAL-148 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTV4NT6wPFkh|ryP MmLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
UACC-812 NX3BbJdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITVbY1KSzVyPUW1PU4{QTFizszN NX\QT5BJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
EW-11 MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTV3Mj6zPVkh|ryP M17mTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
COLO-320-HSR NWL6S5lJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\PTWM2OD13NUGuN|Uh|ryP NFi3Tlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H889 NIG2V4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X2PWlEPTB;NUS3MlI{KM7:TR?= M3XIVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
EVSA-T NITZfXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrXUodKSzVyPUW0N{43QDRizszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
RL M4PK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofwTWM2OD13NEKuOFQzKM7:TR?= MlPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HSC-4 NVnreXRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTV|OT6yPVMh|ryP NF[4fIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H2227 NYjjXVN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTV|MD6yOVQh|ryP NILJNZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NB5 NIL1ZphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLYNVdyUUN3ME21NlYvPDNizszN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H2081 NVjZUWZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K0VWlEPTB;NUK1MlUyOyEQvF2= M2qwNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H510A Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHycYt3UUN3ME21NlQvPjl4IN88US=> NWfhToQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H1436 M{\nXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTV{Mz6wOlQh|ryP MmW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HL-60 M1vq[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LQR2lEPTB;NUKyMlkzPCEQvF2= M1nlOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
Mo-T NVPiVIx2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rHZWlEPTB;NUG1MlEyPiEQvF2= M{DGTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H2171 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTVzMj63NFUh|ryP M2LRW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H1694 Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\nW4V3UUN3ME21NVIvPDN7IN88US=> M{TnTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
P12-ICHIKAWA MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTVzMT60NVYh|ryP M{Du[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
DU-4475 NVTNV5RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fEcWlEPTB;NUGxMlExOSEQvF2= MkXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
RPMI-8402 NXK0TJJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;LTWM2OD13MUCuNFIyKM7:TR?= MnHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
EHEB M2PBWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvsXmRKSzVyPUWwO{4zODhizszN MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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