CHIR-99021 (CT99021)

For research use only.

Catalog No.S1263

475 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 475 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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HAL-01 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PiN2lEPTB;MUKyMlQ6QSEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KYSE-140 NVXsU3hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvnfWpmUUN3ME2xNlIvOTRzIN88US=> MnfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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RT-112 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7R[JpkUUN3ME23MlE3PDV4IN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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BB65-RCC MlqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jNb2lEPTB;Nj61N|E6PSEQvF2= NH\Kemw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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BL-41 NFfvd4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fQe2lEPTB;NT64NVI3PiEQvF2= MnW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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SW1710 M1q0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTiRYpZUUN3ME21MlQzPDV4IN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SK-OV-3 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{juemlEPTB;ND65PVM1KM7:TR?= NFvKZlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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MOLT-16 M{fNOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULBVZdWUUN3ME2zMlg5PTV4IN88US=> M1XnN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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HCC1395 M2HZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVSxd4dHUUN3ME2xMlc5Ojd|IN88US=> NXSz[mNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
MIA-PaCa-2 M2nlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwN{W5O|ch|ryP NEDQWZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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D-247MG NEPa[W9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjKRYM3UUN3ME2wMlk1QDV{IN88US=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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D-336MG NETCTJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULJZWlOUUN3ME2wMlg1PjJizszN MmW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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769-P M2nSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HZVWlEPTB;MD61PFQ6QSEQvF2= M{nxe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
GCT Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrSTWM2OD1yLkOwOlczKM7:TR?= NW\h[W5mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
SW982 NIfEd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEGyc4FKSzVyPUCuNlE1OTZizszN NW\zO256RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ES-CCE NFn6OI9HfW6ldHnvckBCe3OjeR?= MUG1xsDPxE1? M2W1cFMh\A>? NEDBfJZFVVOR NYX0Z3huW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 M2XaVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5N|Y2Lz5{NEe3PVM3PTxxYU6=
ES-D3 MkXPSpVv[3Srb36gRZN{[Xl? NGiyWpc2yqEQvF2= NH\kN4c{KGR? MoHJSG1UVw>? M1zDbXN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? NYfPeJE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-CCE NEmxToREgXSxdH;4bYMhSXO|YYm= NYTqS3FFOTEEoN88US=> MorEN{Bl M3XoTGROW09? NFqxZVRKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? NEm2b|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
ES-D3 NF6yfo9EgXSxdH;4bYMhSXO|YYm= NFLBPG8yOMLizszN M{DKZ|Mh\A>? MUPEUXNQ MUXJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fUB4cXSqIFnDOVAhd2ZiND65JO69VQ>? MlXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{mzOlUoRjJ2N{e5N|Y2RC:jPh?=
Neural progenitor cells NHrlPHVHfW6ldHnvckBCe3OjeR?= NIjY[4g{KM7:TR?= M3[yfVExKGR? M321SWROW09? NV7X[WRPUW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ NY\XN3dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2N|gxOzRpPkK0OlM5ODN2PD;hQi=>
A549 NIHIUlRCeG:ydH;zbZMhSXO|YYm= NVvWSYNVPSEEtV2= NXvjW216OjRiaB?= MVvEUXNQ M4CxdWlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= Mmj6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H157 M2jNSGFxd3C2b4Ppd{BCe3OjeR?= NGC0Z3Q2KML3TR?= M1TuXFI1KGh? NYDrbJRQTE2VTx?= NF62PW9Fd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? Ml7HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H460 MYPBdI9xfG:|aYOgRZN{[Xl? NX7wNnBwPSEEtV2= M4rHflI1KGh? NFLyUG9FVVOR NX63coFiSXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> M4DBNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
H157 M2qxRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HzZVUhyrWP Mn3ZNlQhcA>? NULmS4xITE2VTx?= MmTSVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u NIfXc2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
H460 M1W4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDNNWVIPSEEtV2= MWiyOEBp M3T2XGROW09? NYP6ZWNFWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v NWqwTmlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
embryonic stem cells (ESC) MVvGeY5kfGmxbjDBd5NigQ>? Mlm2N{DDvU1? NXvYPJF[OTFiZB?= Ml:3SG1UVw>? M2LXPHBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= M2WySFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESzN|EzLz5{M{i0N|MyOjxxYU6=
DN3 MWLGeY5kfGmxbjDBd5NigQ>? MVWxNEDPxE1? MWO5OkBp MkPXSG1UVw>? NGTQfYlKdmO{ZXHz[ZMh[2WubDDk[ZZmdG:ybXXueEBidmRicILvcIln\XKjdHnvci=> MnLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3Mk[5PFkoRjJ|NUK2PVg6RC:jPh?=
platelets MoPGSpVv[3Srb36gRZN{[Xl? MYCxNEDPxE1? MVqxOUBucW5? MX\EUXNQ MVvJcoNz\WG|ZYOgeIhzd22kaX6tcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIFHUVEB{\WO{ZYTpc44> NILUcWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVg4Pyd-MkOyN|k5Pzd:L3G+
hiPSC-NPs NXOxb|l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfjN-KBkc7:TR?= NY\2bIUyPzJiaB?= MofsSG1UVw>? NHWxbphKdmO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vyqB? MkPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NEK2PFcoRjJ{NkSyOlg4RC:jPh?=
INS-1E M1[0[2Z2dmO2aX;uJGF{e2G7 M4DodVIvPSEQvF2= MoTCNlQhcA>? MkH1SG1UVw>? NWS5fnlZUW6mdXPld{BiKHKnZIXjeIlwdiCxZjDOVFEhd3[ncnX4dJJme3Orb36= NELVToI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSyO|cxPCd-MkK0Nlc4ODR:L3G+
PANC1 M4[3OmFxd3C2b4Ppd{BCe3OjeR?= NHrSdWbDqDVizszN NHvvOXU4OiCq NUexPVlSTE2VTx?= MlH5WJJq\2encoOgZY4h[XCxcITveIlkKHKnc4DvcpNm NXq3cHpxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFEyQDZpPkKyNlAyOTh4PD;hQi=>
Endothelial cell(EC) Mn;ySpVv[3Srb36gRZN{[Xl? MYGzJO69VQ>? M2e0[WROW09? NVHhfGNpWHKxbX;0[ZMh\W6mb4To[Yxq[WxiY3XscEApTUNrIHTp[oZmemWwdHnheIlwdg>? Ml60QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUKwNFYoRjJ{MEWyNFA3RC:jPh?=
HMC1.2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\NNYQ{OCEQvF2= MVO3NkBp MXrEUXNQ M2G2SnJm\HWlZYOgZ4VtdCC|dYL2bZZidA>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB|OUOwNUc,OjJyM{mzNFE9N2F-
Sca-1+ HPC MnvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPSNkDPxE1? NH7BUG83KGR? NWDn[lczTE2VTx?= Mm[xV5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NXPlfoo5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2NlQ{PDhpPkKxOlI1OzR6PD;hQi=>
Oct4/Sox2/Klf4-infected MEFs NX\SRWxVTnWwY4Tpc44hSXO|YYm= NHq2d|UyOCEQvF2= NHm3PYwzQCCm M3HsW2ROW09? NX\CZ5pQWHKxbX;0[ZMhVUWIczDy[ZBzd2e{YX3tbY5oKFS{YX7z[JVk\WRiYomgU4N1PCxiU3;4Nkwh[W6mIFvs[lQ> NE\a[3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUizPVA2PSd-MUm4N|kxPTV:L3G+
H4IIE MnXRSpVv[3Srb36gRZN{[Xl? MkPlNVAh|ryP NYrFTI5EOjRiaB?= M2HCOmROW09? NGTxN2RT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 NVvFUHZbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzOVAyQTVpPkG1N|UxOTl3PD;hQi=>
insulin receptor–expressing CHO-IR M4DJOWZ2dmO2aX;uJGF{e2G7 MWi1NFAhdk1? NHLi[pg{OCCvaX6= Mo\wSG1UVw>? NFnuRZVC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= NV[yWGxTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2NFY1QTdpPkGyOlA3PDl5PD;hQi=>
3T3-L1 M2\UfWZ2dmO2aX;uJGF{e2G7 MlPSN{DPxE1? NH2zdVQ1KGh? NUD5UWNKTE2VTx?= M2nTZ2lvcGmkaYTzJJBz\WGmaYDvZ5l1\SCmaX\m[ZJmdnSrYYTpc44> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjB3NUKwNEc,OTJyNUWyNFA9N2F-
CHO-IR NVPMTWdVTnWwY4Tpc44hSXO|YYm= MW[zNEBucW5? MWXFR|UxRTBwN{eg{txO M4L6SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MEG2NVIyLz5{OUCxOlEzOTxxYU6=
HepG2 NEe5T21HfW6ldHnvckBCe3OjeR?= NYT6e2JMOyCq NWftZlFvTUN3ME2xMlUh|ryP NVfQe5JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlExOjNpPkKyNlYyODJ|PD;hQi=>

... 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. 

CTNNB1; 

PubMed: 23993102     


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

β-catenin; 

PubMed: 24165128     


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

30709379 23993102 24165128
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
SOX10/EdU; 

PubMed: 28174705     


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

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.

28174705 24779365
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