CHIR-99021 (CT99021) HCl

For research use only.

Catalog No.S2924

374 publications

CHIR-99021 (CT99021) HCl Chemical Structure

CAS No. 1797989-42-4

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

Selleck's CHIR-99021 (CT99021) HCl has been cited by 374 publications

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
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] In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ). [2] Unlike lithium chloride and AR-A014418, CHIR-99021 treatment does not reduce the viability of INS-1E cells even at high concentrations. Instead, CHIR-99021 robustly increases the rate of proliferation of INS-1E cells in a dose-dependent manner, and significantly inhibits INS-E cell death induced by high glucose and high palmitate in a concentration-dependent manner. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 μM, with 2-3 fold increase of cell replication at 5 μM of CHIR-99021 treatment. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 M4P6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTlyMD6yN|Eh|ryP M1LXPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H1155 M3PKcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLDTWM2OD16MUiuNFU6KM7:TR?= NX7HV3pNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
BC-3 MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LTR2lEPTB;OEC1MlIxOyEQvF2= NVLr[It[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
KARPAS-422 M1X3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrnOphXUUN3ME23PFkvOzF3IN88US=> M1HL[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
DEL NXvKeWJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTdyMD64N|gh|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KM-H2 NGfXRoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnPdGNKSzVyPU[5PU4xPTlizszN NXvaRWJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
U-87-MG MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXtTWM2OD14OUSuOVg2KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 NVjjSoI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfVNmlKSzVyPU[5NE4yPzJizszN NGDiNHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-SNU-16 MoP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\MSoRKSzVyPU[4NE41PjJizszN Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
TUR NVK3VVJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTZ5MT6zNlIh|ryP NHPkOVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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L-363 NHXUUXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTZ2OD6wOlQh|ryP NH7r[FM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-H226 M1zS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvmUnB4UUN3ME22NlgvOzV|IN88US=> M4\jXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HT Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTZ{Mj63PFUh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KARPAS-45 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELNTpNKSzVyPU[xPE4zOjFizszN NUf1VlQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ML-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTZyNj61O|kh|ryP Mln6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
LP-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH0TWM2OD14MEOuOVg4KM7:TR?= M{fjWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
L-428 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv2TWM2OD14MECuOlcyKM7:TR?= NEHIOmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
K052 M2PHdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPiRWpKSzVyPUW3PU4zOTNizszN M3;wNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
CAL-148 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTV4NT6wPFkh|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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EW-11 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;kTWM2OD13NUKuN|k6KM7:TR?= M3f1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
COLO-320-HSR NVjPcXc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrsTWM2OD13NUGuN|Uh|ryP MljiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H889 NHf6UJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTV2Nz6yN{DPxE1? Ml\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
EVSA-T M4LtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXiO2c4UUN3ME21OFMvPjh2IN88US=> MonyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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HSC-4 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7OTWM2OD13M{muNlk{KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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NCI-H2081 NGDKOGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\mbGliUUN3ME21NlUvPTF|IN88US=> M3nHZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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TYK-nu MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13lZmlEPTB;MT6wO|kyOiEQvF2= NGrVTlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
D-247MG MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXJTWM2OD1yLkm0PFUzKM7:TR?= NGLXdlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
S-117 NYrnfHl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnNTWM2OD1yLkmyNVMyKM7:TR?= M{PVO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
D-336MG NXX0Z4ZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDCTWM2OD1yLki0OlIh|ryP NVHXfGM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
LOXIMVI NUjjPFd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M131emlEPTB;MD61PFg{OiEQvF2= NXPGR5RIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
769-P M1TnTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwNUi0PVkh|ryP M3\oNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
GCT M321cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4qwU2lEPTB;MD6zNFY4OiEQvF2= NFLaOYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
SW982 M3y5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzVfo9KSzVyPUCuNlE1OTZizszN NWXLcG1DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ES-CCE MYnGeY5kfGmxbjDBd5NigQ>? NGPRfGw2yqEQvF2= NUjHU2o4OyCm MVPEUXNQ MkW2V5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 NInTcGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
ES-D3 MnzmSpVv[3Srb36gRZN{[Xl? MoTDOeKh|ryP NHG4clQ{KGR? NGj0NlZFVVOR MmLCV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 M175SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5N|Y2Lz5{NEe3PVM3PTxxYU6=
ES-CCE NYDyZ202S3m2b4TvfIlkKEG|c3H5 M2rWT|ExyqEQvF2= MVmzJIQ> NEfSdYdFVVOR NITIcIhKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? NU\ZTlRyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-D3 MU\DfZRwfG:6aXOgRZN{[Xl? NFjPOo8yOMLizszN MonFN{Bl M3n0fGROW09? MmjsTY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJkhf2m2aDDJR|UxKG:oIESuPUDPxE1? MoXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{mzOlUoRjJ2N{e5N|Y2RC:jPh?=
Neural progenitor cells M3\BPWZ2dmO2aX;uJGF{e2G7 NV3BO45DOyEQvF2= NUTFPXRIOTBiZB?= NFLvWVVFVVOR NXf0WmpjUW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ MljGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4M{iwN|QoRjJ2NkO4NFM1RC:jPh?=
A549 MXrBdI9xfG:|aYOgRZN{[Xl? M2DkVFUhyrWP MV:yOEBp Mn3OSG1UVw>? M1r0OWlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= NWTCU49bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H157 NUG1Z4JOSXCxcITvd4l{KEG|c3H5 M{jVSVUhyrWP M4rtSlI1KGh? M1;MfWROW09? MVTEc4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> MnmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H460 M4PHTWFxd3C2b4Ppd{BCe3OjeR?= NGm0d|A2KML3TR?= NUXrRYlsOjRiaB?= M2nWbmROW09? NYPkZ3Q3SXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H157 NF3ZZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe1JOK2VQ>? MXuyOEBp NGXVbpVFVVOR NYTrW|RGWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v Mm\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H460 M4PvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjKTm42KML3TR?= MXiyOEBp NEjxUYZFVVOR MYXQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= NX3xXHRpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
embryonic stem cells (ESC) MoPDSpVv[3Srb36gRZN{[Xl? NI\DRYk{KML3TR?= M2fsW|EyKGR? NX3rbm1{TE2VTx?= NUHkXm5EWHKxbX;0[ZMhe2WuZj3y[Y5mf2GuIH;mJI5iy6:4ZT30fZBmKG2xdYPlJIVu[nK7b37pZ{B{fGWvIHPlcIx{KCiHU1Op MkD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NEOzNVIoRjJ|OESzN|EzRC:jPh?=
DN3 MmfjSpVv[3Srb36gRZN{[Xl? NGC2Rm0yOCEQvF2= NEW2bnQ6PiCq MlLHSG1UVw>? M33Fbmlv[3KnYYPld{Bk\WyuIHTleoVtd3CvZX70JIFv\CCycn;sbYZmemG2aX;u MoPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3Mk[5PFkoRjJ|NUK2PVg6RC:jPh?=
platelets M2LHWGZ2dmO2aX;uJGF{e2G7 M1T6XlExKM7:TR?= NWW0dpRJOTVibXnu NHX4fldFVVOR NUnCfGtEUW6lcnXhd4V{KHSqcn;tZolvNW2nZHnheIVlKHCuYYTlcIV1KGGpZ4Ll[4F1cW:wIHHu[EBCXFBic3XjdoV1cW:w NHfoRYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVg4Pyd-MkOyN|k5Pzd:L3G+
hiPSC-NPs MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzGN-KBkc7:TR?= NIniUYs4OiCq MkS2SG1UVw>? M4jPd2lv[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc47DqA>? Mm\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NEK2PFcoRjJ{NkSyOlg4RC:jPh?=
INS-1E M4fMU2Z2dmO2aX;uJGF{e2G7 NWHVT|RsOi53IN88US=> NFP6RYIzPCCq MlHjSG1UVw>? M2DiV2lv\HWlZYOgZUBz\WS3Y4Tpc44hd2ZiTmCxJI93\XKneIDy[ZN{cW:w NH\BR4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSyO|cxPCd-MkK0Nlc4ODR:L3G+
PANC1 NYXxZnNSSXCxcITvd4l{KEG|c3H5 NWHTZXVryqB3IN88US=> MYm3NkBp NHPSeXVFVVOR NGm5SFdVemmpZ3Xyd{BidiCjcH;weI91cWNicnXzdI9ve2V? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyMUG4Okc,OjJ{MEGxPFY9N2F-
Endothelial cell(EC) MYjGeY5kfGmxbjDBd5NigQ>? NFLQfZU{KM7:TR?= Ml;ESG1UVw>? MnPRVJJwdW:2ZYOg[Y5ld3SqZXzpZYwh[2WubDCoSWMqKGSrZn\ldoVvfGmjdHnvci=> NVjNUINmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOVIxODZpPkKyNFUzODB4PD;hQi=>
HMC1.2 NXOwZo9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnnc4RkOzBizszN MnnYO|IhcA>? NFPDe4ZFVVOR MVjS[YR2[2W|IHPlcIwhe3W{dnn2ZYw> NXHtWG46RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwN|k{ODFpPkKyNFM6OzBzPD;hQi=>
Sca-1+ HPC M1Sx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHreJMzKM7:TR?= M2fjUlYh\A>? MlPpSG1UVw>? MVzTfY5memerc4TpZ4FtdHlicILvcY91\XNiU3PhMVEsyqCKUFOgdJJwdGmoZYLheIlwdiCjbnSgZ49td267IH\vdo1ifGmxbjD0c4dmfGincjD3bZRpKEWJRh?= NIXFWpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[yOFM1QCd-MkG2NlQ{PDh:L3G+
Oct4/Sox2/Klf4-infected MEFs M363fWZ2dmO2aX;uJGF{e2G7 M2G1eVExKM7:TR?= MlTFNlgh\A>? NHuzUIRFVVOR NWL3TZhYWHKxbX;0[ZMhVUWIczDy[ZBzd2e{YX3tbY5oKFS{YX7z[JVk\WRiYomgU4N1PCxiU3;4Nkwh[W6mIFvs[lQ> M2L4[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEO5NFU2Lz5zOUizPVA2PTxxYU6=
H4IIE MkLXSpVv[3Srb36gRZN{[Xl? MnjJNVAh|ryP MlqyNlQhcA>? MXrEUXNQ M4nQbnJm\3WuYYTld{DPui2lYYTlcolvKGGldHn2bZR6KGGwZDDUTXJGKGOxboThbY5qdmdicILvcY91\XJiYXP0bZZqfHl? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTN3MEG5OUc,OTV|NUCxPVU9N2F-
insulin receptor–expressing CHO-IR NXjHcpBsTnWwY4Tpc44hSXO|YYm= M1Xu[lUxOCCwTR?= NUfWUIVjOzBibXnu MUfEUXNQ M4OwfWFkfGm4YYTld{BIdHmlb3flckBUgW62aHHz[UApT1Nr NVHKPI1TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2NFY1QTdpPkGyOlA3PDl5PD;hQi=>
3T3-L1 NGXsNpVHfW6ldHnvckBCe3OjeR?= NWG4fXhjOyEQvF2= M{Tle|QhcA>? NYnWdHBtTE2VTx?= NHrrU3ZKdmirYnn0d{BxemWjZHnwc4N6fGViZHnm[oVz\W62aXH0bY9v M1rCdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MEW1NlAxLz5zMkC1OVIxODxxYU6=
CHO-IR NYPHeXI6TnWwY4Tpc44hSXO|YYm= M{jW[VMxKG2rbh?= M{i4NGVEPTB;MD63O{DPxE1? MlrKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlyMU[xNlEoRjJ7MEG2NVIyRC:jPh?=
HepG2 NHjXd|VHfW6ldHnvckBCe3OjeR?= NGrnPWM{KGh? MX7FR|UxRTFwNTFOwG0> NHXSfng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2NVAzOyd-MkKyOlExOjN:L3G+

... 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] Administration of CHIR-99021 significantly augments hematopoietic repopulation in recipient mice transplanted with mouse or human hematopoietic stem cells (HSCs), suggesting that GSK-3 is a specific modulator of HSC activity. [4]

Protocol

Kinase Assay:

[1]

- Collapse

Cell-free kinase assays:

Polypropylene 96-well plates are filled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing 27 nM GSK-3α or 29 nM GSK-3β, and 0.5 μM biotin-CREB peptide substrate. Various concentrations of CHIR-99021 are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a final concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed five times with PBS, filled with 200 μL of scintillation fluid, sealed, left 30 minutes, and counted in a scintillation counter. All steps are performed at room temperature.
Cell Research:

[3]

- Collapse
  • Cell lines: INS-1E
  • Concentrations: Dissolved in DMSO, final concentrations ~ 20 μM
  • Incubation Time: 1, or 4 days
  • Method:

    Cells are maintained for 24 hours in starvation medium (culture medium with only 5 mM glucose, 1% fetal calf serum). Then cells are exposed to various concentrations of CHIR-99021 for 1, or 4 days. Cell number is measured by staining of cellular DNA with CyQuant dye, which becomes fluorescent when bound to DNA. Fluorescence is measured after 30 minutes of incubation using the FLUOstar Optima reader. Cell replication is determined by BrdUrd incorporation. BrdUrd labeling solution is added to the medium for the last 4 hours before the cells are fixed using FixDenat solution and incubated with monoclonal anti-BrdUrd-POD antibodies. After substrate solution is added to each well, the light emission is measured in a microplate luminometer using the Analyst HT detection system.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Female db/db mice or male ZDF rats with type 2 diabetes
  • Dosages: ~48 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (185.33 mM)
Ethanol 2 mg/mL (3.98 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
24mg/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 501.8
Formula

C22H18Cl2N8.HCl

CAS No. 1797989-42-4
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.Cl

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I recently purchased CHIR 99021 to inject mice intraperitoneally. The data sheet says using 10% captisol for in vivo use. Is it for IP injection? Or do you have other solutions to suggest to use for in vivo IP injection of CHIR 99021?

  • Answer:

    The formulation of 15% Captisol is for oral gavage, and S2924 CHIR-99021 (CT99021) HCl in it is a suspension. S2924 CHIR-99021 (CT99021) HCl can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 24mg/ml as a clear solution for IP injection.

  • Question 2:

    How about the half-life of this compound? If it is necessary for daily treatment when the compound is used in long-term experiment?

  • Answer:

    Please change the culture medium each day to add the new comound in it if the duration is more than 72h.

  • Question 3:

    What is the difference between S2924 and S1263? Which one is better for differentiation?

  • Answer:

    S1263 is the free base format of Chir-99021, while S2924 is the HCl salt format. They have the same biological activity but are slightly different in solubility.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID