Laduviglusib (CHIR-99021)

Catalog No.S1263 Synonyms: CT99021

For research use only.

Laduviglusib (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.

Laduviglusib (CHIR-99021) Chemical Structure

CAS No. 252917-06-9

Selleck's Laduviglusib (CHIR-99021) has been cited by 623 publications

Purity & Quality Control

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Biological Activity

Description Laduviglusib (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 NIG3coRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLOfZFKSzVyPUG4Nk43QDhizszN M1HMWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
SN12C NF3Yc5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXVWolKSzVyPUG4Nk45OjlizszN MlPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
A427 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf1TWM2OD1zOESuOlMyKM7:TR?= MlHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
DOK M{TYTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XIbWlEPTB;MUi0MlY1OyEQvF2= NHjGNpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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MRK-nu-1 NIjHTWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXDTWM2OD1zOESuPVczKM7:TR?= NVHSV4gzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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NCI-H1563 M3HSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF6NT6yNFkh|ryP MoLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
MDA-MB-453 NUjsbXhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XzXWlEPTB;MUi2Mlk1OSEQvF2= MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
MONO-MAC-6 M3zGZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTF6Nz6zPVIh|ryP NEDmZW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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SK-LU-1 NHvwSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELvUJBKSzVyPUG4PE41OjhizszN M{XGclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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NCI-H838 NHnQbHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP2UoV2UUN3ME2xPVAvOzRizszN MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
HCE-4 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF7MD65PVIh|ryP NHSxVm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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COLO-668 MoXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLWN2tKSzVyPUG5N{4yPTdizszN M4\5U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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BB30-HNC NVywe4c2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLF[ZI6UUN3ME2xN|QvOTF4IN88US=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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HT-1080 MlXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T0VGlEPTB;MUOyMlIxPCEQvF2= NY\3WJNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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LU-99A MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rhfWlEPTB;MUK5Mlk{OSEQvF2= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
HEC-1 NFnCbI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;OTWM2OD1zMkmuNVk5KM7:TR?= NHfudZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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NCI-H2087 MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjrZWxNUUN3ME2xNlQvOjh|IN88US=> NIG3R5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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OPM-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mne3TWM2OD1zMkOuNVc3KM7:TR?= MmOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
HT-29 Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PWRmlEPTB;MUKyMlc4QCEQvF2= NGmwdpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HAL-01 M1f5OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG4bY5OUUN3ME2xNlIvPDl7IN88US=> NEHufmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
KYSE-140 NFvUXI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXKTWM2OD1zMkKuNVQyKM7:TR?= MontQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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OVCAR-3 MlXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTFzOT65NVUh|ryP M37GfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
KNS-81-FD MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTFzOT60NVch|ryP MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SUP-T1 MofmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;oTWM2OD1zMUiuPVU3KM7:TR?= MnrYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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GCT MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHEWXBIUUN3ME2wMlMxPjd{IN88US=> NXjh[lNwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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ES-CCE M3LE[mZ2dmO2aX;uJGF{e2G7 MlrKOeKh|ryP NFrVT|M{KGR? MWfEUXNQ MVrTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> MnvPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{mzOlUoRjJ2N{e5N|Y2RC:jPh?=
ES-D3 MU\GeY5kfGmxbjDBd5NigQ>? M2T1flXDqM7:TR?= M2TJSFMh\A>? MoDVSG1UVw>? NFLYS41UfHKxbnfsfUBqdmS3Y3XzJJRp\SCjY4Tpeol1gSCxZjDXcpQw[mW2YT3jZZRmdmmwIIDheIh4[Xl? M{f4bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{e5N|Y2Lz5{NEe3PVM3PTxxYU6=
ES-CCE MnPpR5l1d3SxeHnjJGF{e2G7 M4HTSFExyqEQvF2= NX;hcolrOyCm NV\kVZFsTE2VTx?= NUjNPZhwUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHl? NYSyXlNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-D3 MWjDfZRwfG:6aXOgRZN{[Xl? NEflTY4yOMLizszN M2D4blMh\A>? MVPEUXNQ NV35ZZlyUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHlid3n0bEBKSzVyIH;mJFQvQSEQvF2= NH3Kb3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
Neural progenitor cells NVqyXYl4TnWwY4Tpc44hSXO|YYm= MV6zJO69VQ>? NYH0UVFHOTBiZB?= M3HHb2ROW09? NXPHRmtmUW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ MnTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4M{iwN|QoRjJ2NkO4NFM1RC:jPh?=
A549 MV\BdI9xfG:|aYOgRZN{[Xl? NFX2N|Y2KML3TR?= MVGyOEBp M2TVeWROW09? MofETY5kemWjc3XzJINmdGxiYYDvdJRwe2m| NUPqd25GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H157 NG[5RlNCeG:ydH;zbZMhSXO|YYm= MXO1JOK2VQ>? M{jQV|I1KGh? MUjEUXNQ NE\pS3FFd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? NYnDO3pmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H460 MYfBdI9xfG:|aYOgRZN{[Xl? M4exXlUhyrWP NI\xOVMzPCCq MkDBSG1UVw>? MXLBeJRmdnWjdHXzJINmdGxiYYDvdJRwe2m| NITPOWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
H157 NVu5fYpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XwdFUhyrWP M3jjZlI1KGh? M3npbmROW09? M3TzXXBzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> NI\sWGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
H460 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:5fHo2KML3TR?= MUOyOEBp NELHVZRFVVOR MmnPVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u NWK1VoFsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
embryonic stem cells (ESC) NIX5[YZHfW6ldHnvckBCe3OjeR?= NVXXdHc4OyEEtV2= NHTwcVQyOSCm MkDpSG1UVw>? MljuVJJwdW:2ZYOgd4Vt\i2{ZX7le4FtKG:oIH7hx893\S22eYDlJI1wfXOnIHXtZpJ6d26rYzDzeIVuKGOnbHzzJEhGW0Nr M2\JWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESzN|EzLz5{M{i0N|MyOjxxYU6=
DN3 MYXGeY5kfGmxbjDBd5NigQ>? MofDNVAh|ryP NG\ocFI6PiCq Ml:2SG1UVw>? MmnGTY5kemWjc3XzJINmdGxiZHX2[YxweG2nboSgZY5lKHC{b3zp[oVz[XSrb36= NFHX[pM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyOlk5QSd-MkO1NlY6QDl:L3G+
platelets MYDGeY5kfGmxbjDBd5NigQ>? NVXtcXV7OTBizszN NXnwRXlwOTVibXnu Mo\YSG1UVw>? M4qzNGlv[3KnYYPld{B1cHKxbXLpck1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdiCjbnSgRXRRKHOnY4LleIlwdg>? M3XYZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkO5PFc4Lz5{M{KzPVg4PzxxYU6=
hiPSC-NPs M1jiSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmz5qCK|ryP M{XtZVczKGh? MUnEUXNQ Mlf5TY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ2Mk[4O{c,OjJ4NEK2PFc9N2F-
INS-1E MmrWSpVv[3Srb36gRZN{[Xl? MVyyMlUh|ryP M4nU[lI1KGh? NFXYV3VFVVOR MmHoTY5lfWOnczDhJJJm\HWldHnvckBw\iCQUEGgc5ZmemW6cILld5Nqd25? Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2Mke3NFQoRjJ{NEK3O|A1RC:jPh?=
PANC1 NE\mbJJCeG:ydH;zbZMhSXO|YYm= M4P5[:KhPSEQvF2= NHLKVIU4OiCq MUDEUXNQ MnfDWJJq\2encoOgZY4h[XCxcITveIlkKHKnc4DvcpNm NV3FVZVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFEyQDZpPkKyNlAyOTh4PD;hQi=>
Endothelial cell(EC) NEfGS49HfW6ldHnvckBCe3OjeR?= NEnvXm8{KM7:TR?= NVLpeWZYTE2VTx?= NWrNPWNnWHKxbX;0[ZMh\W6mb4To[Yxq[WxiY3XscEApTUNrIHTp[oZmemWwdHnheIlwdg>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB3MkCwOkc,OjJyNUKwNFY9N2F-
HMC1.2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFniTVQ{OCEQvF2= MkPGO|IhcA>? M33hV2ROW09? NY\5UopyWmWmdXPld{Bk\WyuIIP1dpZqfmGu MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB|OUOwNUc,OjJyM{mzNFE9N2F-
Sca-1+ HPC MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\GPIpDOiEQvF2= NU\RbmVRPiCm NGntfI9FVVOR M2\rcHN6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG NVvETHR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2NlQ{PDhpPkKxOlI1OzR6PD;hQi=>
Oct4/Sox2/Klf4-infected MEFs MXfGeY5kfGmxbjDBd5NigQ>? NFLnNGgyOCEQvF2= MXiyPEBl MoHsSG1UVw>? M4G2fnBzd22xdHXzJG1GTnNicnXwdo9oemGvbXnu[{BVemGwc3T1Z4VlKGK7IF;jeFQtKFOxeEKsJIFv\CCNbH[0 MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh|OUC1OUc,OTl6M{mwOVU9N2F-
H4IIE MYjGeY5kfGmxbjDBd5NigQ>? M2fvcFExKM7:TR?= M{\uUlI1KGh? Mnj6SG1UVw>? NH31SFhT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 MmrhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV|NUCxPVUoRjF3M{WwNVk2RC:jPh?=
insulin receptor–expressing CHO-IR Ml[4SpVv[3Srb36gRZN{[Xl? NI\TeXE2ODBibl2= NVXSV45COzBibXnu NVHy[IptTE2VTx?= NG\pRlhC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= NYC2eo9tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2NFY1QTdpPkGyOlA3PDl5PD;hQi=>
3T3-L1 M1yyNGZ2dmO2aX;uJGF{e2G7 NYTGXXY3OyEQvF2= NHrtWow1KGh? NFizO3JFVVOR M3X0SGlvcGmkaYTzJJBz\WGmaYDvZ5l1\SCmaX\m[ZJmdnSrYYTpc44> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjB3NUKwNEc,OTJyNUWyNFA9N2F-
CHO-IR NWLJfZdnTnWwY4Tpc44hSXO|YYm= MXKzNEBucW5? MYLFR|UxRTBwN{eg{txO NWjaWFZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmwNVYyOjFpPkK5NFE3OTJzPD;hQi=>
HepG2 NYPndGg2TnWwY4Tpc44hSXO|YYm= NX63UXFFOyCq MkTzSWM2OD1zLkWg{txO MkixQIEhfGG{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 ; β-catenin ; CTNNB1 30709379 24165128 23993102
Growth inhibition assay Cell viability 22039301
Immunofluorescence Oct3/4 ; SOX10/EdU 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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: Female db/db mice; Male ZDF rats
  • Dosages: 8-48 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 465.34
Formula

C22H18Cl2N8

CAS No. 252917-06-9
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

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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