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409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 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3BTWM2OD17MECuNlMyKM7:TR?= M4ThVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H1155 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjYeo1KSzVyPUixPE4xPTlizszN NX;yeoNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
BC-3 M4j1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T3UGlEPTB;OEC1MlIxOyEQvF2= NGTIRVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
KARPAS-422 M{\vXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPpTWM2OD15OEmuN|E2KM7:TR?= MoPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
DEL MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTdyMD64N|gh|ryP MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KM-H2 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHiU2lKSzVyPU[5PU4xPTlizszN M{jRXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
U-87-MG NXXlSYZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LBfGlEPTB;Nkm0MlU5PSEQvF2= M1rpWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-1 M2\qZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlL1TWM2OD14OUCuNVczKM7:TR?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-16 MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrpWGdKSzVyPU[4NE41PjJizszN M4rJVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
TUR M3HtV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljOTWM2OD14N{GuN|IzKM7:TR?= M{HUOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
IM-9 NFH1OIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTZ3MT61OFEh|ryP M4DIWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
L-363 M2DsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnwZVhKSzVyPU[0PE4xPjRizszN M3vncFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H226 NH7OPIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjTOHVLUUN3ME22NlgvOzV|IN88US=> NXfP[5hERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HT NGKy[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrXRpo3UUN3ME22NlIvPzh3IN88US=> M17E[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KARPAS-45 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HPNGlEPTB;NkG4MlIzOSEQvF2= NW[zTHhURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ML-2 MkDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTZyNj61O|kh|ryP NESzRmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
LP-1 NEL6d5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTZyMz61PFch|ryP MlrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
L-428 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jSdmlEPTB;NkCwMlY4OSEQvF2= M3HkOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
K052 M3jqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu1eolPUUN3ME21O|kvOjF|IN88US=> NULxfoxNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
CAL-148 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jHNGlEPTB;NU[1MlA5QSEQvF2= M2m5blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
UACC-812 M3zIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fUZWlEPTB;NUW5MlM6OSEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
EW-11 NHzadGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL5TZVGUUN3ME21OVIvOzl7IN88US=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
COLO-320-HSR MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTV3MT6zOUDPxE1? M2ezeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H889 M4\6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DjUmlEPTB;NUS3MlI{KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
EVSA-T Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe2dGRKSzVyPUW0N{43QDRizszN NHTZZnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
RL MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTV2Mj60OFIh|ryP MoDaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HSC-4 NUTDc4dbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTV|OT6yPVMh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H2227 M1T5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTV|MD6yOVQh|ryP NULvb4JlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NB5 M1nleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y4NmlEPTB;NUK2MlQ{KM7:TR?= M4PyU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H2081 MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HMO2lEPTB;NUK1MlUyOyEQvF2= NETuelk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H510A NIjlOVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\Ve2lEPTB;NUK0MlY6PiEQvF2= Mn\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1436 NEfGZo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULMcmV6UUN3ME21NlMvODZ2IN88US=> NVG5d5kxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HL-60 NV7QRoN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoCyTWM2OD13MkKuPVI1KM7:TR?= NV\obI9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
Mo-T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTFVnR{UUN3ME21NVUvOTF4IN88US=> M3XSSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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NCI-H1694 Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTVzMj60N|kh|ryP M4[wXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
P12-ICHIKAWA MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLpToNJUUN3ME21NVEvPDF4IN88US=> M4T5fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
DU-4475 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[1Tnd7UUN3ME21NVEvOTBzIN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
RPMI-8402 NUXSTGMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHJXZI5UUN3ME21NVAvODJzIN88US=> MnjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
EHEB NHrsOlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTVyNz6yNFgh|ryP MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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