CHIR-99021 (CT99021)

For research use only.

Catalog No.S1263

519 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.

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Selleck's CHIR-99021 (CT99021) has been cited by 519 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
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SN12C NVzJOFFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHBfJNoUUN3ME2xPFIvQDJ7IN88US=> M1Pq[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
A427 NHXBXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\wOHdKSzVyPUG4OE43OzFizszN MnPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
DOK NUPuTpJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7XTWM2OD1zOESuOlQ{KM7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
MDA-MB-415 M4T0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTF6ND62OVEh|ryP NInEOmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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HCE-4 NYTJZXFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXi0dnJ[UUN3ME2xPVAvQTl{IN88US=> MlOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
A2780 Ml;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETGbHVKSzVyPUG5Nk45QTFizszN NIe1OXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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JVM-3 NU\4eo9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLpTWM2OD1zOUiuOFE6KM7:TR?= M4jYTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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CTB-1 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jx[WlEPTB;MUOyMlg6PyEQvF2= M3TJeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HT-1080 Mnv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTF|Mj6yNFQh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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HEC-1 NXnYV4dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT4TWM2OD1zMkmuNVk5KM7:TR?= M1O5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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UMC-11 Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv6TWM2OD1zMk[uNFM5KM7:TR?= NIe5WoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H2087 NInwXIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLQTWM2OD1zMkSuNlg{KM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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OPM-2 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M131Z2lEPTB;MUKzMlE4PiEQvF2= Mn3aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HT-29 NWjsSGpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;iTWM2OD1zMkKuO|c5KM7:TR?= M1S3TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HAL-01 NYHGNGM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrNT2dTUUN3ME2xNlIvPDl7IN88US=> M2jv[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KYSE-140 NVi5NIJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrYcFlmUUN3ME2xNlIvOTRzIN88US=> NHXaUng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HuP-T4 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPvU5NKSzVyPUGyNU42PSEQvF2= NW\sNIZLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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MEG-01 M2DLbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XmWWlEPTB;OD65PVA1OyEQvF2= Mk\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
MKN28 NFSy[29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XSZWlEPTB;OD64PFUyPiEQvF2= MkjMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
CAL-72 MnXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRThwN{[xNVMh|ryP NVf3W2doRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
MV-4-11 NYPkcpJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX2XWN4UUN3ME24MlU1OzB2IN88US=> NHmySWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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RT-112 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfBcop5UUN3ME23MlE3PDV4IN88US=> MmD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
CAL-85-1 M3Pqcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPPN3NIUUN3ME22MlYxQTN4IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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LB2518-MEL NH;lWZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PrOmlEPTB;NT63NlYzPyEQvF2= NF3LTmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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NCI-H2452 MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\GTWM2OD13LkS1OlI5KM7:TR?= M1W1O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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MHH-ES-1 M3jMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:w[WlEPTB;ND6wOFU1PSEQvF2= M2DaUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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MOLT-16 Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNwOEi1OVYh|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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HOP-62 NITFRWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfBdJA4UUN3ME2zMlM3ODV2IN88US=> NX3rVnVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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NCI-H2122 NHvQUVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG1TWM2OD1{LkK3Olg1KM7:TR?= M17w[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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TYK-nu MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m0R2lEPTB;MT6wO|kyOiEQvF2= Mnm4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
D-247MG NIfzT3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\BTWM2OD1yLkm0PFUzKM7:TR?= M3XRT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
S-117 M2PEU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwOUKxN|Eh|ryP NWrZXlJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
D-336MG M{\jNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K3cWlEPTB;MD64OFYzKM7:TR?= NGC2OIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
LOXIMVI NFHBeHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W2fWlEPTB;MD61PFg{OiEQvF2= NEjxdpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
769-P MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;3SVBKSzVyPUCuOVg1QTlizszN NHXNRWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
GCT M4fPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr3V4hHUUN3ME2wMlMxPjd{IN88US=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SW982 M2i4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkOyTWM2OD1yLkKxOFE3KM7:TR?= Ml;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
ES-CCE NVLnfodSTnWwY4Tpc44hSXO|YYm= NYXqbWNYPcLizszN NFjyPVE{KGR? MV3EUXNQ MlfQV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 NXXN[nZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-D3 MXLGeY5kfGmxbjDBd5NigQ>? NGi4PJg2yqEQvF2= MoXUN{Bl MUTEUXNQ NXPrVIFSW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 M2\xSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5N|Y2Lz5{NEe3PVM3PTxxYU6=
ES-CCE MWPDfZRwfG:6aXOgRZN{[Xl? M{TwPFExyqEQvF2= MnvRN{Bl NEfwS2JFVVOR NETDNXpKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
ES-D3 Mn60R5l1d3SxeHnjJGF{e2G7 M4j6cVExyqEQvF2= NVzsXIxbOyCm NXO0bVJ5TE2VTx?= NVnpWoYyUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHlid3n0bEBKSzVyIH;mJFQvQSEQvF2= M2jlZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5N|Y2Lz5{NEe3PVM3PTxxYU6=
Neural progenitor cells NIrDTGtHfW6ldHnvckBCe3OjeR?= M4nQSlMh|ryP MmTDNVAh\A>? M17jXGROW09? NGrsTlFKdmS3Y3XzJIdmdmW{YYTpc44hd2ZibnX1doFtKHC{b3flcol1d3JiY3XscJM> MlLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4M{iwN|QoRjJ2NkO4NFM1RC:jPh?=
A549 MmDJRZBweHSxc3nzJGF{e2G7 M{XHNFUhyrWP M1riTlI1KGh? MYnEUXNQ NIC3ZZNKdmO{ZXHz[ZMh[2WubDDhdI9xfG:|aYO= M2HafVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
H157 M3rDemFxd3C2b4Ppd{BCe3OjeR?= M4ns[FUhyrWP MnXRNlQhcA>? MkDNSG1UVw>? MWLEc4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H460 NF[2RnNCeG:ydH;zbZMhSXO|YYm= NIXzd3M2KML3TR?= MljjNlQhcA>? M4Ln[GROW09? NUPTbJBnSXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H157 MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYe1JOK2VQ>? NVy2cGk2OjRiaB?= NWryN5RFTE2VTx?= NGjudFJRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> NXnFcXRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H460 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[1JOK2VQ>? MnzJNlQhcA>? M4n0SGROW09? NGi5S|BRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> M4K2S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
embryonic stem cells (ESC) NXviV|NpTnWwY4Tpc44hSXO|YYm= MY[zJOK2VQ>? NYn1WYZNOTFiZB?= NXXycWhZTE2VTx?= NYPWUIw6WHKxbX;0[ZMhe2WuZj3y[Y5mf2GuIH;mJI5iy6:4ZT30fZBmKG2xdYPlJIVu[nK7b37pZ{B{fGWvIHPlcIx{KCiHU1Op NX\oPGxqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFM{OTJpPkKzPFQ{OzF{PD;hQi=>
DN3 Ml35SpVv[3Srb36gRZN{[Xl? NEO1R4QyOCEQvF2= NH:1Wo46PiCq NWKxOWtuTE2VTx?= MUHJcoNz\WG|ZYOgZ4VtdCCmZY\lcI9xdWWwdDDhcoQheHKxbHnm[ZJifGmxbh?= NVLNUlVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlY6QDlpPkKzOVI3QTh7PD;hQi=>
platelets MoXnSpVv[3Srb36gRZN{[Xl? NHrIPYEyOCEQvF2= NIPGbIUyPSCvaX6= Ml\wSG1UVw>? NVvCZok4UW6lcnXhd4V{KHSqcn;tZolvNW2nZHnheIVlKHCuYYTlcIV1KGGpZ4Ll[4F1cW:wIHHu[EBCXFBic3XjdoV1cW:w MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OUi3O{c,OjN{M{m4O|c9N2F-
hiPSC-NPs M123XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP1N-KBkc7:TR?= MX63NkBp MUHEUXNQ M16wTmlv[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc47DqA>? M2WwdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkSyOlg4Lz5{Mk[0NlY5PzxxYU6=
INS-1E NYLXSVViTnWwY4Tpc44hSXO|YYm= M1PV[lIvPSEQvF2= Mn\3NlQhcA>? NX;CWG96TE2VTx?= M3rWbGlv\HWlZYOgZUBz\WS3Y4Tpc44hd2ZiTmCxJI93\XKneIDy[ZN{cW:w NUPwN|FSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0Nlc4ODRpPkKyOFI4PzB2PD;hQi=>
PANC1 MoTLRZBweHSxc3nzJGF{e2G7 MkfOxsA2KM7:TR?= M4DvdVczKGh? NYHtS283TE2VTx?= MVnUdolo\2W{czDhckBieG:ydH;0bYMhemW|cH;ud4U> MlnrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MEGxPFYoRjJ{MkCxNVg3RC:jPh?=
Endothelial cell(EC) MoDkSpVv[3Srb36gRZN{[Xl? NGXiWZo{KM7:TR?= NFGyR3NFVVOR NYHQ[FdxWHKxbX;0[ZMh\W6mb4To[Yxq[WxiY3XscEApTUNrIHTp[oZmemWwdHnheIlwdg>? NH24do89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC1NlAxPid-MkKwOVIxODZ:L3G+
HMC1.2 M3LucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzTTnlqOzBizszN MXS3NkBp NYLoW5pTTE2VTx?= MoXrVoVlfWOnczDj[YxtKHO3co\peoFt MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB|OUOwNUc,OjJyM{mzNFE9N2F-
Sca-1+ HPC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;NbFczKM7:TR?= NWPFTVBbPiCm M3TTemROW09? MWXTfY5memerc4TpZ4FtdHlicILvcY91\XNiU3PhMVEsyqCKUFOgdJJwdGmoZYLheIlwdiCjbnSgZ49td267IH\vdo1ifGmxbjD0c4dmfGincjD3bZRpKEWJRh?= NEXnOZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[yOFM1QCd-MkG2NlQ{PDh:L3G+
Oct4/Sox2/Klf4-infected MEFs NEnwOmtHfW6ldHnvckBCe3OjeR?= NXjpTHR{OTBizszN M{LKSFI5KGR? MnTWSG1UVw>? MVrQdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= NHLWe4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUizPVA2PSd-MUm4N|kxPTV:L3G+
H4IIE MnqxSpVv[3Srb36gRZN{[Xl? MnHMNVAh|ryP NWjGPWVHOjRiaB?= Ml64SG1UVw>? MmjGVoVofWyjdHXzJO6zNWOjdHXubY4h[WO2aY\peJkh[W6mIGTJVmUh[2:wdHHpcolv\yCycn;tc5RmeiCjY4Tpeol1gQ>? NHLnWng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUO1NFE6PSd-MUWzOVAyQTV:L3G+
insulin receptor–expressing CHO-IR NHS4ZVFHfW6ldHnvckBCe3OjeR?= NFLFdWg2ODBibl2= MnnjN|AhdWmw NIjyXZZFVVOR MlnkRYN1cX[jdHXzJGdtgWOxZ3XuJHN6dnSqYYPlJEhIWyl? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZyNkS5O{c,OTJ4ME[0PVc9N2F-
3T3-L1 NFraPGdHfW6ldHnvckBCe3OjeR?= MUmzJO69VQ>? NFK1NnU1KGh? NFvub|ZFVVOR NVn0T3pxUW6qaXLpeJMheHKnYXTpdI9kgXSnIHTp[oZmemWwdHnheIlwdg>? M13JVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MEW1NlAxLz5zMkC1OVIxODxxYU6=
CHO-IR NWTybYxbTnWwY4Tpc44hSXO|YYm= MVizNEBucW5? NVzrcJFiTUN3ME2wMlc4KM7:TR?= NIPqNZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUCxOlEzOSd-MkmwNVYyOjF:L3G+
HepG2 NF;4eWdHfW6ldHnvckBCe3OjeR?= M3XW[|MhcA>? NGj0NY5GSzVyPUGuOUDPxE1? M3GyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[xNFI{Lz5{MkK2NVAzOzxxYU6=

... 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