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 635 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 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnleZVKSzVyPUG4Nk43QDhizszN M4rTWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
SN12C MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jlemlEPTB;MUiyMlgzQSEQvF2= NHTDblk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
A427 NH3scplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPReFhZUUN3ME2xPFQvPjNzIN88US=> MkTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
DOK NIqxNJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXz1eXhRUUN3ME2xPFQvPjR|IN88US=> M3n1[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
MDA-MB-415 NVLGO3R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF6ND62OVEh|ryP NH\FO|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
MRK-nu-1 NUjNR|dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;0RnZ4UUN3ME2xPFQvQTd{IN88US=> MmPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
LB2241-RCC M{\iR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrFNFBKSzVyPUG4OU4yPDVizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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MDA-MB-453 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\KZ4FKSzVyPUG4Ok46PDFizszN MojkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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NCI-H838 NF7XOFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K5NGlEPTB;MUmwMlM1KM7:TR?= NGjwRWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
HCE-4 NYLpfJE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLOTWM2OD1zOUCuPVkzKM7:TR?= MnzBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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KOSC-2 Ml\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF7NT64NVgh|ryP MkjFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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RT-112 NHPF[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGxfo5HUUN3ME23MlE3PDV4IN88US=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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BB65-RCC M3fyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTZwNUOxPVUh|ryP M4Hkd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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LB2518-MEL NEnmZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluxTWM2OD13LkeyOlI4KM7:TR?= Mlq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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RCC10RGB NEH6WW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDzSHZKSzVyPUSuNlk1PzlizszN NYHacJZZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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S-117 NY\mfJBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r1XGlEPTB;MD65NlE{OSEQvF2= NGDncmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
D-336MG MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwOES2NkDPxE1? NVPXSnBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
LOXIMVI NInBR25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz1TWM2OD1yLkW4PFMzKM7:TR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
769-P NIjwS4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jlb2lEPTB;MD61PFQ6QSEQvF2= NEnmemw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
GCT MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHnTWM2OD1yLkOwOlczKM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SW982 M3X5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfEbXFKSzVyPUCuNlE1OTZizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
ES-CCE MVjGeY5kfGmxbjDBd5NigQ>? M1jIZVXDqM7:TR?= NX3n[5luOyCm NEfWS3ZFVVOR NInzdoFUfHKxbnfsfUBqdmS3Y3XzJJRp\SCjY4Tpeol1gSCxZjDXcpQw[mW2YT3jZZRmdmmwIIDheIh4[Xl? NE\kSWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
ES-D3 NFXxPFlHfW6ldHnvckBCe3OjeR?= NXrWV4xrPcLizszN NGOwWo0{KGR? NX;n[ml{TE2VTx?= MoTaV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 MlXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{mzOlUoRjJ2N{e5N|Y2RC:jPh?=
ES-CCE MnvwR5l1d3SxeHnjJGF{e2G7 M4TvNFExyqEQvF2= NILMc3c{KGR? MWjEUXNQ M4f5fGlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6 NEXyXGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
ES-D3 NWnIdGN[S3m2b4TvfIlkKEG|c3H5 MUexNOKh|ryP M1jpflMh\A>? M2H4SGROW09? NITKWnpKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gSC5aYToJGlEPTBib3[gOE46KM7:TR?= NGjHemI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
Neural progenitor cells NEKzV3hHfW6ldHnvckBCe3OjeR?= NFrT[nk{KM7:TR?= NFnhWpkyOCCm NH;RNYFFVVOR M{m5RWlv\HWlZYOg[4Vv\XKjdHnvckBw\iCwZYXyZYwheHKxZ3XubZRweiClZXzsdy=> NVXJWYpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2N|gxOzRpPkK0OlM5ODN2PD;hQi=>
A549 NHH2b5pCeG:ydH;zbZMhSXO|YYm= M3yxUVUhyrWP NFjZfHUzPCCq MnjTSG1UVw>? M1ntWmlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= NGXmWm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
H157 MYrBdI9xfG:|aYOgRZN{[Xl? M{XKWlUhyrWP MVuyOEBp NEDlW|JFVVOR M4fGd2Rw\XNibn;0JJNq\26rZnnjZY51dHliYX\m[YN1KGGyb4D0c5Nqew>? NV\UZWNURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlc3QDhpPkK0N|Y4Pjh6PD;hQi=>
H460 MWTBdI9xfG:|aYOgRZN{[Xl? M{XGNlUhyrWP M4nVPFI1KGh? MkDYSG1UVw>? NECyeWxCfHSnboXheIV{KGOnbHygZZBweHSxc3nz MmS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H157 NVzqfZBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PuO|UhyrWP MX2yOEBp MnnJSG1UVw>? MXPQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H460 M3yxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3uZWg3PSEEtV2= NUniRlc5OjRiaB?= MV\EUXNQ MWTQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= NHjrNnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
embryonic stem cells (ESC) NWXBVVFpTnWwY4Tpc44hSXO|YYm= MmfGN{DDvU1? NUH5UmhOOTFiZB?= NFTDWpRFVVOR M4W5WHBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= NYPUbnBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFM{OTJpPkKzPFQ{OzF{PD;hQi=>
DN3 MoXSSpVv[3Srb36gRZN{[Xl? MYixNEDPxE1? MXW5OkBp NGq4dnJFVVOR MoDvTY5kemWjc3XzJINmdGxiZHX2[YxweG2nboSgZY5lKHC{b3zp[oVz[XSrb36= MlLnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3Mk[5PFkoRjJ|NUK2PVg6RC:jPh?=
platelets M{i4bWZ2dmO2aX;uJGF{e2G7 NEK3XIoyOCEQvF2= Moq2NVUhdWmw MW\EUXNQ NXX5PHY5UW6lcnXhd4V{KHSqcn;tZolvNW2nZHnheIVlKHCuYYTlcIV1KGGpZ4Ll[4F1cW:wIHHu[EBCXFBic3XjdoV1cW:w MoH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{m4O|coRjJ|MkO5PFc4RC:jPh?=
hiPSC-NPs M3TFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmz5qCK|ryP MWG3NkBp M1fuemROW09? MVjJcoNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uxsA> NX;Fb2RmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OFI3QDdpPkKyOlQzPjh5PD;hQi=>
INS-1E NFXN[XdHfW6ldHnvckBCe3OjeR?= MWeyMlUh|ryP NVe2[5Z{OjRiaB?= NXfwellOTE2VTx?= MYXJcoR2[2W|IHGgdoVlfWO2aX;uJI9nKE6SMTDveoVz\XiycnXzd4lwdg>? NHvm[5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSyO|cxPCd-MkK0Nlc4ODR:L3G+
PANC1 NVPPTFhDSXCxcITvd4l{KEG|c3H5 NIjpcILDqDVizszN MlnvO|IhcA>? NXPVPVU6TE2VTx?= NUTiZXpvXHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn NVG5SpNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFEyQDZpPkKyNlAyOTh4PD;hQi=>
Endothelial cell(EC) MlzmSpVv[3Srb36gRZN{[Xl? MUSzJO69VQ>? NW\6d3U5TE2VTx?= MkDHVJJwdW:2ZYOg[Y5ld3SqZXzpZYwh[2WubDCoSWMqKGSrZn\ldoVvfGmjdHnvci=> NU\nOWhTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwOVIxODZpPkKyNFUzODB4PD;hQi=>
HMC1.2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHxbXNkOzBizszN MnP3O|IhcA>? M3HPV2ROW09? MVHS[YR2[2W|IHPlcIwhe3W{dnn2ZYw> NYnZV|BSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwN|k{ODFpPkKyNFM6OzBzPD;hQi=>
Sca-1+ HPC M2fRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;PRWgzKM7:TR?= NUPTO4JIPiCm NX3xbFBFTE2VTx?= MkG3V5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NEfvVno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[yOFM1QCd-MkG2NlQ{PDh:L3G+
Oct4/Sox2/Klf4-infected MEFs M3LsVGZ2dmO2aX;uJGF{e2G7 NUDnSmV1OTBizszN Mlr5Nlgh\A>? NXv0eItLTE2VTx?= MlvpVJJwdW:2ZYOgUWVHeyC{ZYDyc4dz[W2vaX7nJHRz[W6|ZIXj[YQh[nliT3P0OEwhW2:6MjygZY5lKEuuZkS= NWT6WmplRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4N|kxPTVpPkG5PFM6ODV3PD;hQi=>
H4IIE MUjGeY5kfGmxbjDBd5NigQ>? MWCxNEDPxE1? NFXMN5gzPCCq M3\t[2ROW09? M{PFb3Jm\3WuYYTld{DPui2lYYTlcolvKGGldHn2bZR6KGGwZDDUTXJGKGOxboThbY5qdmdicILvcY91\XJiYXP0bZZqfHl? Ml:wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV|NUCxPVUoRjF3M{WwNVk2RC:jPh?=
insulin receptor–expressing CHO-IR Mkm4SpVv[3Srb36gRZN{[Xl? M3XUT|UxOCCwTR?= Mn7oN|AhdWmw MmrsSG1UVw>? MkjkRYN1cX[jdHXzJGdtgWOxZ3XuJHN6dnSqYYPlJEhIWyl? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZyNkS5O{c,OTJ4ME[0PVc9N2F-
3T3-L1 NXzJU|BtTnWwY4Tpc44hSXO|YYm= Mk\0N{DPxE1? NYHWR|RqPCCq NUfuT|JvTE2VTx?= NETUN41KdmirYnn0d{BxemWjZHnwc4N6fGViZHnm[oVz\W62aXH0bY9v NFTwflk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkC1OVIxOCd-MUKwOVUzODB:L3G+
CHO-IR NIXzNm9HfW6ldHnvckBCe3OjeR?= NXXVbnIyOzBibXnu NGW2eJFGSzVyPUCuO|ch|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTBzNkGyNUc,OjlyMU[xNlE9N2F-
HepG2 NV\x[mhFTnWwY4Tpc44hSXO|YYm= NE[1N4g{KGh? MWPFR|UxRTFwNTFOwG0> NYfIb25QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlExOjNpPkKyNlYyODJ|PD;hQi=>
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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