CHIR-99021 (CT99021)

For research use only.

Catalog No.S1263

553 publications

CHIR-99021 (CT99021) Chemical Structure

CAS No. 252917-06-9

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

Selleck's CHIR-99021 (CT99021) has been cited by 553 publications

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Choose Selective GSK-3 Inhibitors

Biological Activity

Description CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
In vitro

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LOUCY MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHicXRZUUN3ME2xPFIvPjh6IN88US=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SN12C MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITLdFJKSzVyPUG4Nk45OjlizszN NEjDeGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
A427 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi1OZdwUUN3ME2xPFQvPjNzIN88US=> NXL2[XZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
DOK MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT5VowyUUN3ME2xPFQvPjR|IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
MDA-MB-415 M3TGSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjjeGZwUUN3ME2xPFQvPjVzIN88US=> NYjSSFNVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
MRK-nu-1 NIPVUGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXCTWM2OD1zOESuPVczKM7:TR?= Ml7OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
LB2241-RCC NGeyfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXryOoJDUUN3ME2xPFUvOTR3IN88US=> MmqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1563 NXPUT3VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jtU2lEPTB;MUi1MlIxQSEQvF2= NVPEVGF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
MDA-MB-453 NEnDUmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TvWmlEPTB;MUi2Mlk1OSEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
MONO-MAC-6 M{HOWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2G1WWlEPTB;MUi3MlM6OiEQvF2= NYeydno6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
CAPAN-1 NETFcIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfIfZJ5UUN3ME2xPFcvPDV|IN88US=> M2PlNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
SK-LU-1 NWXzbpJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF6OD60Nlgh|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H1299 M2XkO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fJc2lEPTB;MUi4MlcyQSEQvF2= Mlv4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KG-1 NHzFVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17zdGlEPTB;MUi5Mlc6QCEQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
ETK-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rrTGlEPTB;MUmwMlE5OSEQvF2= M{HkPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H838 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzlO3BJUUN3ME2xPVAvOzRizszN MknWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HCE-4 M{P1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHSTWM2OD1zOUCuPVkzKM7:TR?= NGnrd2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
A2780 NFr5ZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[3WpNKSzVyPUG5Nk45QTFizszN MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
COLO-668 M2TscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HqTWlEPTB;MUmzMlE2PyEQvF2= NInsbnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HGC-27 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTF7NT61N|gh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SW1088 MmPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVToZlZmUUN3ME2xPVUvPjd5IN88US=> MkXlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KOSC-2 NIjyTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjYTWM2OD1zOUWuPFE5KM7:TR?= NILFepY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
SW780 M2PIUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPFblFyUUN3ME2xPVYvPzN2IN88US=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
TE-1 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LXcmlEPTB;MUm2MlI3KM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
22RV1 NV:3[pVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDlbVE1UUN3ME2xPVcvPDJ2IN88US=> NF;sXWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
IA-LM NUK1eXc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m3c2lEPTB;MUm3MlgzOiEQvF2= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
TE-5 NHzVT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKwW4IyUUN3ME2xPVgvODN|IN88US=> NVHod5lRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
JVM-3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjwTWM2OD1zOUiuOFE6KM7:TR?= M1X6T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HT55 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLhTWM2OD1zOUmuNVkzKM7:TR?= NEjZN2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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SJRH30 NVjh[2dFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJyMD61NVUh|ryP NVn0[I9rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
COLO-679 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7kSIdKSzVyPUKwNE45PTlizszN NUHTfoxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
MFM-223 M1yy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrLepl{UUN3ME2yNFEvPTh5IN88US=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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Detroit562 NXnMcYY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLOepFVUUN3ME2xOFEvPDZ4IN88US=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
OVCAR-4 NFnKNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPYTWM2OD1zNECuO|Q6KM7:TR?= Ml\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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NOS-1 NETmcVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnWzTWM2OD1zM{SuO|Y2KM7:TR?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-H1437 NGiye|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULpNoUyUUN3ME2xN|QvPTlizszN NF\FUJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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HT-1080 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HmdWlEPTB;MUOyMlIxPCEQvF2= MmXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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UMC-11 MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzITWM2OD1zMk[uNFM5KM7:TR?= NXnQT3k6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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HT-29 M1HCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGmzeZpKSzVyPUGyNk44PzhizszN NWTm[2ttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HAL-01 M4PkeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF{Mj60PVkh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KYSE-140 Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jubGlEPTB;MUKyMlE1OSEQvF2= NI\qN3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HuP-T4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[5NmlEPTB;MUKxMlU2KM7:TR?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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OVCAR-3 MoXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jSfGlEPTB;MUG5MlkyPSEQvF2= NYHrNYQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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SUP-T1 M3fmUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTiTWM2OD1zMUiuPVU3KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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BB65-RCC MlnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzxTWM2OD14LkWzNVk2KM7:TR?= MlHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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SK-OV-3 NFLrdnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTRwOUmzOEDPxE1? MoruQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
ALL-PO M2X4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHGbWZRUUN3ME20Mlg{QDV6IN88US=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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RCC10RGB M2LNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjYTWM2OD12LkK5OFc6KM7:TR?= M3PMVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NKM-1 NEjJc4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TUNGlEPTB;ND6xN|k4OSEQvF2= MlXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
MHH-ES-1 M2\1TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYm1bmFYUUN3ME20MlA1PTR3IN88US=> MoTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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MOLT-16 NFGzZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj6ZVVqUUN3ME2zMlg5PTV4IN88US=> M3vqUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
A172 NGPmfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXwNppKSzVyPUOuO|U1QThizszN NV[0R45DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HCC1569 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zMc2lEPTB;Mz60PFMxPSEQvF2= MnfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HOP-62 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLjTWM2OD1|LkO2NFU1KM7:TR?= NWq4dG1uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
A704 M4r4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnlTWM2OD1|LkC4NVIh|ryP NFTGXoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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RPMI-7951 NFf6[3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXFN3NKSzVyPUKuO|AyQTNizszN M{XvVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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HCC1395 NHLlRm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\yd5g{UUN3ME2xMlc5Ojd|IN88US=> Mlf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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KYSE-180 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwN{K3PFgh|ryP MknaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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GCT NHzzfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj6OXh5UUN3ME2wMlMxPjd{IN88US=> M3PiXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
SW982 NH;mbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwMkG0NVYh|ryP M1LQTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
ES-CCE NHS0PIVHfW6ldHnvckBCe3OjeR?= NWm1[nQ1PcLizszN MVGzJIQ> MlHoSG1UVw>? MXXTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
ES-D3 MnOySpVv[3Srb36gRZN{[Xl? NGPzVYc2yqEQvF2= MYOzJIQ> NYW5cnVtTE2VTx?= MYLTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> NVG3XXp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-CCE Mk\sR5l1d3SxeHnjJGF{e2G7 MnfZNVDDqM7:TR?= MV6zJIQ> NGXRPZhFVVOR NFrvXlRKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
ES-D3 NXf0SoYzS3m2b4TvfIlkKEG|c3H5 NFzuco4yOMLizszN NGXWVWI{KGR? MVTEUXNQ NInjTYdKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gSC5aYToJGlEPTBib3[gOE46KM7:TR?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
Neural progenitor cells MWLGeY5kfGmxbjDBd5NigQ>? NEPFS3M{KM7:TR?= MWGxNEBl M3uwRmROW09? NE\LOJhKdmS3Y3XzJIdmdmW{YYTpc44hd2ZibnX1doFtKHC{b3flcol1d3JiY3XscJM> MlztQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4M{iwN|QoRjJ2NkO4NFM1RC:jPh?=
A549 MYrBdI9xfG:|aYOgRZN{[Xl? NIDpTFk2KML3TR?= NF\NOm0zPCCq MY\EUXNQ M17Z[Wlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= M{f4cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
H157 NEXrfZFCeG:ydH;zbZMhSXO|YYm= NEHPTVg2KML3TR?= M2HtOlI1KGh? M1rD[WROW09? NVX4dWFSTG:nczDuc5Qhe2mpbnnmbYNidnSueTDh[oZm[3RiYYDvdJRwe2m| NX3H[2JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H460 Mm\ORZBweHSxc3nzJGF{e2G7 Ml20OUDDvU1? MlTvNlQhcA>? NXXPcpdmTE2VTx?= MnzsRZR1\W63YYTld{Bk\WyuIHHwc5B1d3Orcx?= MnK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H157 M1fmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXy1JOK2VQ>? NVfv[o5VOjRiaB?= M13XbWROW09? MYfQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= M3PqUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
H460 NY\LOlhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHpWIc2KML3TR?= NWTXblBYOjRiaB?= NGm5elhFVVOR Mm\IVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u M1nDSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
embryonic stem cells (ESC) NGrSc4RHfW6ldHnvckBCe3OjeR?= M{nmW|MhyrWP NF\PbIgyOSCm NYDZS5VQTE2VTx?= M3fyd3Bzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NEOzNVIoRjJ|OESzN|EzRC:jPh?=
DN3 M2jIVmZ2dmO2aX;uJGF{e2G7 MUCxNEDPxE1? M3PzZVk3KGh? Mn\5SG1UVw>? NEiwb4dKdmO{ZXHz[ZMh[2WubDDk[ZZmdG:ybXXueEBidmRicILvcIln\XKjdHnvci=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV{Nkm4PUc,OjN3Mk[5PFk9N2F-
platelets NXvtTmF{TnWwY4Tpc44hSXO|YYm= MXexNEDPxE1? NXj0cGw6OTVibXnu MWLEUXNQ NFOxOmhKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? NWDGUGYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyN|k5PzdpPkKzNlM6QDd5PD;hQi=>
hiPSC-NPs M1;QRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXiz5qCK|ryP NVHE[Zd6PzJiaB?= NWPYd2VTTE2VTx?= NWjU[3BzUW6lcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdsLi MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ2Mk[4O{c,OjJ4NEK2PFc9N2F-
INS-1E MWLGeY5kfGmxbjDBd5NigQ>? NXmxUYVQOi53IN88US=> M3rMTVI1KGh? NHzZfItFVVOR NEfqNHdKdmS3Y3XzJIEhemWmdXP0bY9vKG:oIF7QNUBwfmW{ZYjwdoV{e2mxbh?= MorVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2Mke3NFQoRjJ{NEK3O|A1RC:jPh?=
PANC1 MVHBdI9xfG:|aYOgRZN{[Xl? MnLVxsA2KM7:TR?= NIiyfXk4OiCq NUTmeVhsTE2VTx?= M3W2VnRzcWepZYLzJIFvKGGyb4D0c5Rq[yC{ZYPwc45{\Q>? NV6zRXQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFEyQDZpPkKyNlAyOTh4PD;hQi=>
Endothelial cell(EC) NFmxcXpHfW6ldHnvckBCe3OjeR?= NVr0e3pROyEQvF2= NWjWPWNWTE2VTx?= MWHQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u MmOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUKwNFYoRjJ{MEWyNFA3RC:jPh?=
HMC1.2 NGXiS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF74ZpY{OCEQvF2= NGnCNnM4OiCq MXjEUXNQ MkLTVoVlfWOnczDj[YxtKHO3co\peoFt MmrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyM{mzNFEoRjJ{MEO5N|AyRC:jPh?=
Sca-1+ HPC NEHMbHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXBb45HOiEQvF2= NFnFc|g3KGR? M1jHfGROW09? NW\YO3dHW3mwZYLnbZN1cWOjbHz5JJBzd22xdHXzJHNk[S1zK9MgTHBEKHC{b3zp[oVz[XSrb36gZY5lKGOxbH;ufUBnd3KvYYTpc44hfG:pZYTo[ZIhf2m2aDDFS2Y> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTZ{NEO0PEc,OjF4MkSzOFg9N2F-
Oct4/Sox2/Klf4-infected MEFs NEPMRWVHfW6ldHnvckBCe3OjeR?= MYCxNEDPxE1? NHjRO|UzQCCm NYHYW2d3TE2VTx?= MV7Qdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= NWDIUlU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4N|kxPTVpPkG5PFM6ODV3PD;hQi=>
H4IIE NXfjVWJuTnWwY4Tpc44hSXO|YYm= NYSwVIxbOTBizszN MmnENlQhcA>? MUXEUXNQ MVrS[Yd2dGG2ZYOg{tIu[2G2ZX7pckBi[3Srdnn0fUBidmRiVFnSSUBkd262YXnubY5oKHC{b33veIVzKGGldHn2bZR6 NYnaXmN2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzOVAyQTVpPkG1N|UxOTl3PD;hQi=>
insulin receptor–expressing CHO-IR MmjmSpVv[3Srb36gRZN{[Xl? NE\WeGM2ODBibl2= NEP0NXg{OCCvaX6= NF7aO4RFVVOR NV;BdWdRSWO2aY\heIV{KEeueXPv[4VvKFO7boToZZNmKCiJUzm= NYPwNXY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2NFY1QTdpPkGyOlA3PDl5PD;hQi=>
3T3-L1 MlfISpVv[3Srb36gRZN{[Xl? NIDyfYM{KM7:TR?= M1nBWVQhcA>? NXvie3RnTE2VTx?= MUTJcohq[mm2czDwdoVi\Gmyb3P5eIUh\GmoZnXy[Y51cWG2aX;u MlfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJyNUWyNFAoRjF{MEW1NlAxRC:jPh?=
CHO-IR M2jXXGZ2dmO2aX;uJGF{e2G7 MnntN|AhdWmw MYPFR|UxRTBwN{eg{txO NUjVPFh4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwNVYyOjFpPkK5NFE3OTJzPD;hQi=>
HepG2 NFHVT49HfW6ldHnvckBCe3OjeR?= M2XQeVMhcA>? M3jHOmVEPTB;MT61JO69VQ>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4MUCyN{c,OjJ{NkGwNlM9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

30709379 24165128 23993102
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3-30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

SOX10/EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

24779365 28174705
In vivo Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge[1].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: Insulin receptor–expressing CHO-IR cells; Primary rat hepatocytes
  • Concentrations: 0.01-10 μM
  • Incubation Time: 30 min
  • Method:

    CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 ml of medium without fetal bovine serum. After 24 h, medium is replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37°C. Cells are lysed and centrifuged 15 min at 4°C/14000g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mmol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Female db/db mice; Male ZDF rats
  • Dosages: 8-48 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL warmed (21.48 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
3.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.34
Formula

C22H18Cl2N8

CAS No. 252917-06-9
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID