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289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 NHz3T5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDibVZRUUN3ME25NFAvOjNzIN88US=> NU\CSmFuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H1155 M132cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRThzOD6wOVkh|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
BC-3 M2K2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHheo1uUUN3ME24NFUvOjB|IN88US=> NVOw[Y16RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
KARPAS-422 NFzKTnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHSOYs6UUN3ME23PFkvOzF3IN88US=> M1fYT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
DEL M2f5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYq4WYU6UUN3ME23NFAvQDN6IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KM-H2 M1PKUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTZ7OT6wOVkh|ryP NHjNNWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
U-87-MG M1TlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTZ7ND61PFUh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 NWrqeIRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\JTWM2OD14OUCuNVczKM7:TR?= M2LHU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-16 M1P0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jaSGlEPTB;NkiwMlQ3OiEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
TUR MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jkXmlEPTB;NkexMlMzOiEQvF2= NH\CfmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
IM-9 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HwdWlEPTB;NkWxMlU1OSEQvF2= M1fhOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
L-363 MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHm0fFNKSzVyPU[0PE4xPjRizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H226 MmL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkezTWM2OD14MkiuN|U{KM7:TR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
HT MljrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLuTWM2OD14MkKuO|g2KM7:TR?= M2qyWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KARPAS-45 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITCTWtKSzVyPU[xPE4zOjFizszN NVHQO29ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ML-2 NWnySYRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P0T2lEPTB;NkC2MlU4QSEQvF2= NWXLV25RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
LP-1 Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LhcWlEPTB;NkCzMlU5PyEQvF2= Mlu0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
L-428 M3L1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnq2TWM2OD14MECuOlcyKM7:TR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
K052 NIfNNo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fjSmlEPTB;NUe5MlIyOyEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
CAL-148 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPmTWM2OD13NkWuNFg6KM7:TR?= NUP5UIlXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
UACC-812 NGfIXlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3qyPGlEPTB;NUW5MlM6OSEQvF2= NHrxXJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
EW-11 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjEWYhKSzVyPUW1Nk4{QTlizszN NFe5bo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
COLO-320-HSR MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnleHBKSzVyPUW1NU4{PSEQvF2= M{DWTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H889 NVrYOmdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\VTWM2OD13NEeuNlMh|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
EVSA-T NUnudItuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTV2Mz62PFQh|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
RL MnrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTV2Mj60OFIh|ryP NHPYW449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HSC-4 NELKc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrwPIVQUUN3ME21N|kvOjl|IN88US=> NH;yNmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H2227 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3mcmlKSzVyPUWzNE4zPTRizszN NWXUNWVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NB5 NICzc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33nOmlEPTB;NUK2MlQ{KM7:TR?= M3\NTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H2081 NFP0OIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;4XmlEPTB;NUK1MlUyOyEQvF2= NGHoVlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H510A NULScmF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\hPYtKSzVyPUWyOE43QTZizszN MkDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1436 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjTfZRmUUN3ME21NlMvODZ2IN88US=> NVLjTmhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HL-60 NH;UXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3kfHhTUUN3ME21NlIvQTJ2IN88US=> NES3Xmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
Mo-T M{jhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTVzNT6xNVYh|ryP M1LzSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H2171 NYniUoRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n5UWlEPTB;NUGyMlcxPSEQvF2= NWfDSGFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H1694 M3G4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHqTWM2OD13MUKuOFM6KM7:TR?= NUe5VFJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
P12-ICHIKAWA MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLOZm5KSzVyPUWxNU41OTZizszN M375TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
DU-4475 M3vETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGwUJBKSzVyPUWxNU4yODFizszN MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
RPMI-8402 M1jJUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XTPWlEPTB;NUGwMlAzOSEQvF2= NIXVOW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
EHEB MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTVyNz6yNFgh|ryP NGfyVWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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