CHIR-99021 (CT99021) HCl

Catalog No.S2924

For research use only.

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.

CHIR-99021 (CT99021) HCl Chemical Structure

CAS No. 1797989-42-4

Selleck's CHIR-99021 (CT99021) HCl has been cited by 405 publications

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Other GSK-3 Products

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 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTlyMD6yN|Eh|ryP Mn[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H1155 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRThzOD6wOVkh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
BC-3 M1vZO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRThyNT6yNFMh|ryP MoDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KARPAS-422 M2nLU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvzbYFpUUN3ME23PFkvOzF3IN88US=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
DEL NX:zWlBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTdyMD64N|gh|ryP M2PPZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KM-H2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm0TWM2OD14OUmuNFU6KM7:TR?= M1L6RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
U-87-MG MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTZ7ND61PFUh|ryP NHH5e4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-SNU-1 NV3RW|diT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL4bYdKSzVyPU[5NE4yPzJizszN MlrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-SNU-16 NH\wUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF33RXlKSzVyPU[4NE41PjJizszN MnXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
TUR M33jW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fjOmlEPTB;NkexMlMzOiEQvF2= NVy0NoZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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L-363 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTZ2OD6wOlQh|ryP Mn;3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H226 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\IeGFCUUN3ME22NlgvOzV|IN88US=> NXSxXGRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
HT NGnsUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTZ{Mj63PFUh|ryP MoTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KARPAS-45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPtOplxUUN3ME22NVgvOjJzIN88US=> NYDob3JuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ML-2 NWfjXoQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17nS2lEPTB;NkC2MlU4QSEQvF2= MmjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
LP-1 NV3qVWt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KyUGlEPTB;NkCzMlU5PyEQvF2= NX3zUZM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
L-428 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3n6N2lEPTB;NkCwMlY4OSEQvF2= M{HsSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
K052 M3HXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrMVVNHUUN3ME21O|kvOjF|IN88US=> NXPRR21qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
CAL-148 NX:0b5Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTV4NT6wPFkh|ryP Mlm1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
UACC-812 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnpSmdIUUN3ME21OVkvOzlzIN88US=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
EW-11 NFvTdVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLPUm5KSzVyPUW1Nk4{QTlizszN NHXKZnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
COLO-320-HSR MkjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTV3MT6zOUDPxE1? NXvE[VdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
NCI-H889 NVrCV3hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\UdmNKSzVyPUW0O{4zOyEQvF2= MmDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
EVSA-T NWi5TmF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILHVGpKSzVyPUW0N{43QDRizszN MlHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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HSC-4 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn2cpFKSzVyPUWzPU4zQTNizszN M{TxZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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NCI-H2081 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\Xc2lEPTB;NUK1MlUyOyEQvF2= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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769-P M2H6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTKTWM2OD1yLkW4OFk6KM7:TR?= M2PtOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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ES-CCE NVnZfIp7TnWwY4Tpc44hSXO|YYm= M3XwXlXDqM7:TR?= M2iwWFMh\A>? M4PHO2ROW09? NH\JR4JUfHKxbnfsfUBqdmS3Y3XzJJRp\SCjY4Tpeol1gSCxZjDXcpQw[mW2YT3jZZRmdmmwIIDheIh4[Xl? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
ES-D3 NUjwZWNtTnWwY4Tpc44hSXO|YYm= M3voTlXDqM7:TR?= M{nLT|Mh\A>? M{j2PGROW09? MnryV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 NWjVcXA5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-CCE MXTDfZRwfG:6aXOgRZN{[Xl? M37P[|ExyqEQvF2= NGH1VmU{KGR? M2r1dWROW09? NEfWOmNKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? MnriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{mzOlUoRjJ2N{e5N|Y2RC:jPh?=
ES-D3 MXrDfZRwfG:6aXOgRZN{[Xl? MXqxNOKh|ryP M3PyOlMh\A>? MlXhSG1UVw>? NYTw[2tKUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHlid3n0bEBKSzVyIH;mJFQvQSEQvF2= NFXnTXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
Neural progenitor cells MnXUSpVv[3Srb36gRZN{[Xl? NFj6TmE{KM7:TR?= NGDvcVcyOCCm MYnEUXNQ NVPuSZB{UW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ NFvIRYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[zPFA{PCd-MkS2N|gxOzR:L3G+
A549 MUHBdI9xfG:|aYOgRZN{[Xl? NIm4cZA2KML3TR?= NUnrc|I2OjRiaB?= NXSz[XZFTE2VTx?= Ml\KTY5kemWjc3XzJINmdGxiYYDvdJRwe2m| Mk\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H157 M330U2Fxd3C2b4Ppd{BCe3OjeR?= MYq1JOK2VQ>? NU\1RpV{OjRiaB?= M1TmSmROW09? NVLab4Q2TG:nczDuc5Qhe2mpbnnmbYNidnSueTDh[oZm[3RiYYDvdJRwe2m| MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H460 NELpWFdCeG:ydH;zbZMhSXO|YYm= NFW3dnE2KML3TR?= NXTYc4VHOjRiaB?= NEm5ZmZFVVOR M2TlRWF1fGWwdXH0[ZMh[2WubDDhdI9xfG:|aYO= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H157 M4S5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi1JOK2VQ>? NGHyWnAzPCCq M4PxWmROW09? NGrHcHJRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> MorKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H460 NGfaZZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDuSoE2KML3TR?= NUfWRol4OjRiaB?= NHTxWVNFVVOR MYjQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= NWj3O|BCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
embryonic stem cells (ESC) NVjmWGpnTnWwY4Tpc44hSXO|YYm= M2\qdlMhyrWP NFTwTIoyOSCm MYrEUXNQ M2T6NnBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= NGW4coo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i0N|MyOid-MkO4OFM{OTJ:L3G+
DN3 Mo\0SpVv[3Srb36gRZN{[Xl? MmnBNVAh|ryP M4fnVlk3KGh? NYrmOmcxTE2VTx?= MXzJcoNz\WG|ZYOgZ4VtdCCmZY\lcI9xdWWwdDDhcoQheHKxbHnm[ZJifGmxbh?= M1n0R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUK2PVg6Lz5{M{WyOlk5QTxxYU6=
platelets NV24T|l6TnWwY4Tpc44hSXO|YYm= NEnSNHkyOCEQvF2= NF7KWWkyPSCvaX6= M2XNSGROW09? NF\NNXJKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? M4XFPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFc4Lz5{M{KzPVg4PzxxYU6=
hiPSC-NPs M2\hdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{GyT|PjiIoQvF2= NUO4ZpROPzJiaB?= MXTEUXNQ NYfSc5BbUW6lcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdsLi NXPo[HVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OFI3QDdpPkKyOlQzPjh5PD;hQi=>
INS-1E MnOwSpVv[3Srb36gRZN{[Xl? MnOzNk42KM7:TR?= M36zd|I1KGh? NYjLfnpYTE2VTx?= MVXJcoR2[2W|IHGgdoVlfWO2aX;uJI9nKE6SMTDveoVz\XiycnXzd4lwdg>? MkTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2Mke3NFQoRjJ{NEK3O|A1RC:jPh?=
PANC1 MVTBdI9xfG:|aYOgRZN{[Xl? NGj4bmrDqDVizszN M17yR|czKGh? MWnEUXNQ M2i0THRzcWepZYLzJIFvKGGyb4D0c5Rq[yC{ZYPwc45{\Q>? NFTGcnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwNVE5Pid-MkKyNFEyQDZ:L3G+
Endothelial cell(EC) MlG1SpVv[3Srb36gRZN{[Xl? MYizJO69VQ>? MnvISG1UVw>? MUnQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u MkXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyNUKwNFYoRjJ{MEWyNFA3RC:jPh?=
HMC1.2 NUHIdZpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWzNEDPxE1? NGfsXWk4OiCq NFfKVJlFVVOR NX;KOmtNWmWmdXPld{Bk\WyuIIP1dpZqfmGu NUDR[4tWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwN|k{ODFpPkKyNFM6OzBzPD;hQi=>
Sca-1+ HPC NIrzWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVqzd4hqOiEQvF2= MkPoOkBl Mn3TSG1UVw>? MlPBV5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NV;P[2hkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2NlQ{PDhpPkKxOlI1OzR6PD;hQi=>
Oct4/Sox2/Klf4-infected MEFs Mkj1SpVv[3Srb36gRZN{[Xl? MXuxNEDPxE1? MYSyPEBl MUHEUXNQ NEL5cXlRem:vb4Tld{BOTU[|IILldJJw\3KjbX3pcochXHKjboPkeYNm\CCkeTDPZ5Q1NCCVb4iyMEBidmRiS3zmOC=> NFvRcJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUizPVA2PSd-MUm4N|kxPTV:L3G+
H4IIE NVXSWFE{TnWwY4Tpc44hSXO|YYm= M1zoTFExKM7:TR?= M33nNFI1KGh? Ml64SG1UVw>? NIS4VFFT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 M{LDfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{WwNVk2Lz5zNUO1NFE6PTxxYU6=
insulin receptor–expressing CHO-IR M3qxcGZ2dmO2aX;uJGF{e2G7 MXK1NFAhdk1? NGK1dGw{OCCvaX6= NXrNcG95TE2VTx?= M{SwemFkfGm4YYTld{BIdHmlb3flckBUgW62aHHz[UApT1Nr MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZyNkS5O{c,OTJ4ME[0PVc9N2F-
3T3-L1 NVfpe|RJTnWwY4Tpc44hSXO|YYm= MWCzJO69VQ>? NH\Ed3o1KGh? NF\ldXFFVVOR MYHJcohq[mm2czDwdoVi\Gmyb3P5eIUh\GmoZnXy[Y51cWG2aX;u MnLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJyNUWyNFAoRjF{MEW1NlAxRC:jPh?=
CHO-IR MX;GeY5kfGmxbjDBd5NigQ>? NX;rTG1pOzBibXnu NISxUotGSzVyPUCuO|ch|ryP M36yOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MEG2NVIyLz5{OUCxOlEzOTxxYU6=
HepG2 NVfrV3B2TnWwY4Tpc44hSXO|YYm= MnywN{Bp Ml;GSWM2OD1zLkWg{txO MlL1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkGwNlMoRjJ{Mk[xNFI{RC:jPh?=
Assay
Methods Test Index PMID
Western blot Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin ; CTNNB1 ; β-catenin 30709379 23993102 24165128
Growth inhibition assay Cell viability 22039301
Immunofluorescence SOX10 / EdU ; Oct3/4 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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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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