CHIR-99021 (CT99021) HCl

For research use only.

Catalog No.S2924

173 publications

CHIR-99021 (CT99021) HCl Chemical Structure

Molecular Weight(MW): 501.8

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.

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Selleck's CHIR-99021 (CT99021) HCl has been cited by 173 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
3T3-L1 NHvENW5HfW6ldHnvckBCe3OjeR?= NFf2O4o{KM7:TR?= Mmi2OEBp NGPaPYpFVVOR M2TLWWlvcGmkaYTzJJBz\WGmaYDvZ5l1\SCmaX\m[ZJmdnSrYYTpc44> NITxTJUyOjB3NUKwNC=>
insulin receptor–expressing CHO-IR NYPmSGI1TnWwY4Tpc44hSXO|YYm= MmLzOVAxKG6P NVSwfXZ7OzBibXnu NWLnRmkxTE2VTx?= NFLGdGFC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= NV[5VXNIOTJ4ME[0PVc>
H4IIE MVLGeY5kfGmxbjDBd5NigQ>? NGLMWnIyOCEQvF2= NUDpToJsOjRiaB?= MkjISG1UVw>? M3vRcnJm\3WuYYTld{DPui2lYYTlcolvKGGldHn2bZR6KGGwZDDUTXJGKGOxboThbY5qdmdicILvcY91\XJiYXP0bZZqfHl? MWOxOVM2ODF7NR?=
Oct4/Sox2/Klf4-infected MEFs NUjvfYJ7TnWwY4Tpc44hSXO|YYm= NXW4SJpIOTBizszN M2PvUlI5KGR? MU\EUXNQ MXXQdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= NXrFVlVoOTl6M{mwOVU>
Sca-1+ HPC MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoP4NkDPxE1? Mm\DOkBl NEfaT4hFVVOR NIfMUlFUgW6ncnfpd5Rq[2GubImgdJJwdW:2ZYOgV4NiNTFtwrDIVGMheHKxbHnm[ZJifGmxbjDhcoQh[2:ub375JIZwem2jdHnvckB1d2endHjldkB4cXSqIFXHSi=> M{nJe|IyPjJ2M{S4
HMC1.2 NGrRRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPuTGc{OCEQvF2= M{fkXlczKGh? NVjPPFJ1TE2VTx?= NWr6VVhlWmWmdXPld{Bk\WyuIIP1dpZqfmGu MXuyNlA{QTNyMR?=
Endothelial cell(EC) NFPEV|RHfW6ldHnvckBCe3OjeR?= NH\3VpI{KM7:TR?= M{j0SmROW09? M{nEOXBzd22xdHXzJIVv\G:2aHXsbYFtKGOnbHygLGVEMSCmaX\m[ZJmdnSrYYTpc44> MmTMNlIxPTJyME[=
PANC1 NY\xcohZSXCxcITvd4l{KEG|c3H5 MoXPxsA2KM7:TR?= M1nmblczKGh? NXvHSoVZTE2VTx?= M322PXRzcWepZYLzJIFvKGGyb4D0c5Rq[yC{ZYPwc45{\Q>? NWSzRpFJOjJ{MEGxPFY>
INS-1E MXzGeY5kfGmxbjDBd5NigQ>? MnHiNk42KM7:TR?= M2TNZlI1KGh? NX3L[odPTE2VTx?= M3zh[2lv\HWlZYOgZUBz\WS3Y4Tpc44hd2ZiTmCxJI93\XKneIDy[ZN{cW:w NEnDdXMzOjR{N{ewOC=>
hiPSC-NPs MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HzVFPjiIoQvF2= Mn7jO|IhcA>? NWrzWGxETE2VTx?= MUjJcoNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;uxsA> MYWyNlY1OjZ6Nx?=
platelets M2XjT2Z2dmO2aX;uJGF{e2G7 M1naTFExKM7:TR?= MXexOUBucW5? M4L4RWROW09? NX;KVodKUW6lcnXhd4V{KHSqcn;tZolvNW2nZHnheIVlKHCuYYTlcIV1KGGpZ4Ll[4F1cW:wIHHu[EBCXFBic3XjdoV1cW:w NGfU[5MzOzJ|OUi3Oy=>
DN3 NH:3NIVHfW6ldHnvckBCe3OjeR?= M1fGVlExKM7:TR?= NXW3W2dEQTZiaB?= M4HZPGROW09? MUDJcoNz\WG|ZYOgZ4VtdCCmZY\lcI9xdWWwdDDhcoQheHKxbHnm[ZJifGmxbh?= NULSV4RDOjN3Mk[5PFk>
embryonic stem cells (ESC) MlLHSpVv[3Srb36gRZN{[Xl? NX7lWHdoOyEEtV2= NUnGcZh2OTFiZB?= NITwWGNFVVOR NVL4doVmWHKxbX;0[ZMhe2WuZj3y[Y5mf2GuIH;mJI5iy6:4ZT30fZBmKG2xdYPlJIVu[nK7b37pZ{B{fGWvIHPlcIx{KCiHU1Op NXG1cXV7OjN6NEOzNVI>
H460 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfMOUDDvU1? M{PRVVI1KGh? NXzaTmg5TE2VTx?= MUfQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= MYiyOFM3PzZ6OB?=
H157 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v3[lUhyrWP MlKyNlQhcA>? NGqxT25FVVOR M{HkV3Bzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> NWjRXJVoOjR|Nke2PFg>
H460 MlfJRZBweHSxc3nzJGF{e2G7 NWG4eVdzPSEEtV2= M{TZWlI1KGh? NXT2c2NDTE2VTx?= MnPNRZR1\W63YYTld{Bk\WyuIHHwc5B1d3Orcx?= NYq2dVl7OjR|Nke2PFg>
H157 Mof1RZBweHSxc3nzJGF{e2G7 NF;zfHc2KML3TR?= MWqyOEBp NFjiSVJFVVOR MX7Ec4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> NYD1OWlwOjR|Nke2PFg>
A549 MXnBdI9xfG:|aYOgRZN{[Xl? M2rwOlUhyrWP MmLFNlQhcA>? NUDvVWhDTE2VTx?= MUHJcoNz\WG|ZYOgZ4VtdCCjcH;weI9{cXN? MnXWNlQ{Pjd4OEi=
Neural progenitor cells NVLoN5J2TnWwY4Tpc44hSXO|YYm= NWG4WJlGOyEQvF2= MojyNVAh\A>? NV3pcmNjTE2VTx?= MnHoTY5lfWOnczDn[Y5memG2aX;uJI9nKG6ndYLhcEBxem:pZX7peI9zKGOnbHzz NEi2fW4zPDZ|OECzOC=>
ES-D3 MWjDfZRwfG:6aXOgRZN{[Xl? NFHJNocyOMLizszN NH7BS2k{KGR? NEPaSpNFVVOR MXXJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fUB4cXSqIFnDOVAhd2ZiND65JO69VQ>? NVH0em9sOjR5N{mzOlU>
ES-CCE NFnQUphEgXSxdH;4bYMhSXO|YYm= Ml\iNVDDqM7:TR?= NYjFU4MyOyCm NE\wWGpFVVOR M1PW[Wlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6 NIrlZWwzPDd5OUO2OS=>
ES-D3 MnjzSpVv[3Srb36gRZN{[Xl? MkX1OeKh|ryP NYXK[ZFZOyCm M3m1UGROW09? NUfMempmW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 MmLrNlQ4Pzl|NkW=
ES-CCE MmS5SpVv[3Srb36gRZN{[Xl? MlLpOeKh|ryP MmLpN{Bl NEHTN5RFVVOR NXLObpMyW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 M2HjPFI1Pzd7M{[1
SW982 NHXqXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TqZWlEPTB;MD6yNVQyPiEQvF2= MmjqV2FPT0WU
GCT M3XUb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTBwM{C2O|Ih|ryP MULTRW5ITVJ?
769-P MmfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDCdnpKSzVyPUCuOVg1QTlizszN Mn\PV2FPT0WU
LOXIMVI NUjQS|U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwNUi4N|Ih|ryP NVPzRYVKW0GQR1XS
D-336MG M13EWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDnTWM2OD1yLki0OlIh|ryP Mnq5V2FPT0WU
S-117 M3TNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTUNWFKSzVyPUCuPVIyOzFizszN M1;LVnNCVkeHUh?=
D-247MG NIDIV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrOOGhKSzVyPUCuPVQ5PTJizszN MWTTRW5ITVJ?
TYK-nu NGTpSYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqySZVKSzVyPUGuNFc6OTJizszN MXzTRW5ITVJ?
A498 NYLzTnpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jEW2lEPTB;MT6zNFQ3QSEQvF2= MoLUV2FPT0WU
BCPAP NGTWNFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIK1cIxKSzVyPUGuOlY5QThizszN NFe1[ZhUSU6JRWK=
KYSE-180 NVjNT|Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K4[WlEPTB;MT63Nlc5QCEQvF2= NIfIZnJUSU6JRWK=
MIA-PaCa-2 NGHPUllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzLNJp4UUN3ME2xMlc2QTd5IN88US=> Mmi0V2FPT0WU
HCC1395 NGDxUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLGTWM2OD1zLke4Nlc{KM7:TR?= MYfTRW5ITVJ?
RS4-11 NYrLVIlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrLW3lnUUN3ME2xMlk2PDF3IN88US=> NF74OIhUSU6JRWK=
NCI-H2122 NYW3foI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvOfHBlUUN3ME2yMlI4Pjh2IN88US=> M33TNHNCVkeHUh?=
SNU-423 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJwNEm3PFch|ryP NWi5cmZDW0GQR1XS
SK-LMS-1 NHz3PJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETmUoZKSzVyPUKuOlQyOjhizszN MUDTRW5ITVJ?
RPMI-7951 MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3wNVNKSzVyPUKuO|AyQTNizszN MUHTRW5ITVJ?
COLO-829 NUfQSo9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLBZmhIUUN3ME2yMlc3PTRizszN MoG4V2FPT0WU
SCC-9 NXfaOI91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJwOUW0PFUh|ryP MXnTRW5ITVJ?
A704 NFPKb4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNwMEixNkDPxE1? NH3nUZNUSU6JRWK=
HOP-62 NGW1b5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnHZml[UUN3ME2zMlM3ODV2IN88US=> MYnTRW5ITVJ?
HCC1569 M4r1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XoOWlEPTB;Mz60PFMxPSEQvF2= NH35TGJUSU6JRWK=
A172 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTNwN{W0PVgh|ryP MWPTRW5ITVJ?
MOLT-16 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPGNVVKSzVyPUOuPFg2PTZizszN NG[2clFUSU6JRWK=
TE-15 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\2fHZpUUN3ME2zMlk2OzR|IN88US=> MX7TRW5ITVJ?
OE19 NVruZ2tMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTNwOU[0OVEh|ryP NVTpVJVXW0GQR1XS
MHH-ES-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLwTWM2OD12LkC0OVQ2KM7:TR?= MmfkV2FPT0WU
NKM-1 M124Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfuSYdKSzVyPUSuNVM6PzFizszN MUjTRW5ITVJ?
RCC10RGB Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTRwMkm0O|kh|ryP NX3TSmVzW0GQR1XS
BxPC-3 NYPuUIRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDHSnZKSzVyPUSuO|A{QTFizszN NHnYcHhUSU6JRWK=
ALL-PO NHvmW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:4WlR1UUN3ME20Mlg{QDV6IN88US=> NIL2WndUSU6JRWK=
SK-OV-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTRwOUmzOEDPxE1? Mn:2V2FPT0WU
SW1710 NGCxWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTVwNEK0OVYh|ryP MmT6V2FPT0WU
NCI-H2452 NHHRWJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HZTGlEPTB;NT60OVYzQCEQvF2= MmjHV2FPT0WU
D-392MG MoP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\uR2lEPTB;NT60PVE1PSEQvF2= NVnJOGxVW0GQR1XS
LB2518-MEL M3f2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHzfY9KSzVyPUWuO|I3OjdizszN MWXTRW5ITVJ?
BL-41 M3uzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELob|BKSzVyPUWuPFEzPjZizszN MnjlV2FPT0WU
WM-115 M1L1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTVwOEG1NFkh|ryP MmnsV2FPT0WU
SK-MEL-2 M16yTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HUTGlEPTB;Nj6zPFM1PCEQvF2= MVzTRW5ITVJ?
CGTH-W-1 NVPhWoFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz3W3VKSzVyPU[uOFE4KM7:TR?= NI\oenRUSU6JRWK=
BB65-RCC MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPz[I9tUUN3ME22MlU{OTl3IN88US=> MnjKV2FPT0WU
CAL-85-1 NXLnW5d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTZwNkC5N|Yh|ryP MlLhV2FPT0WU
RT-112 M1;rR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7iepRIUUN3ME23MlE3PDV4IN88US=> MoTjV2FPT0WU
MC116 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTdwMki2PVEh|ryP NEThV4pUSU6JRWK=
G-361 NEjiU3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTwV5lKSzVyPUeuOFY2PjFizszN MW\TRW5ITVJ?
SW1417 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTdwNkS1PFQh|ryP M3jW[XNCVkeHUh?=
MV-4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3QXmZKSzVyPUiuOVQ{ODRizszN NXfy[lZlW0GQR1XS
CAL-72 NGPFcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fDfGlEPTB;OD63OlEyOyEQvF2= NET1N4tUSU6JRWK=
MKN28 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTqPGpKSzVyPUiuPFg2OTZizszN M33RT3NCVkeHUh?=
MEG-01 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;1eZV6UUN3ME24Mlk6ODR|IN88US=> MlLsV2FPT0WU
ACHN NF7Ye|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;uTWM2OD17LkOwOVQ3KM7:TR?= M4nVfnNCVkeHUh?=
NCI-H1755 NVP1PWJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTlwM{m5PFYh|ryP MnvpV2FPT0WU
NCI-H64 MojiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTlwNEKyOVUh|ryP NUnydopTW0GQR1XS
COLO-205 NY\Q[5NIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn36TWM2OD17LkSzPFIyKM7:TR?= M1jSdHNCVkeHUh?=
CTV-1 M1HvbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj3TWM2OD17LkSzPFk1KM7:TR?= MVHTRW5ITVJ?
U-2-OS MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K1RmlEPTB;OT60OVAxPiEQvF2= NVjOSWc3W0GQR1XS
LB996-RCC M1jaeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTlwNUKzPVch|ryP MUPTRW5ITVJ?
SK-N-DZ NHfqRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn4[XJ{UUN3ME25MlY2PzR{IN88US=> M2PjZ3NCVkeHUh?=
EFM-19 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\CTWM2OD17Lke1OVY3KM7:TR?= NHfQPIdUSU6JRWK=
DBTRG-05MG MkXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTNT4E6UUN3ME25Mlc4PzdizszN MljHV2FPT0WU
U-118-MG MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuxboxKSzVyPUmuPVQ1PDRizszN MlLQV2FPT0WU
LB1047-RCC MkLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi3TWM2OD17Lkm5O|k5KM7:TR?= Mn\hV2FPT0WU
NCI-H28 M2\KZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfFV5VKSzVyPUGwMlQ1OTNizszN NXTaPIwzW0GQR1XS
MZ2-MEL MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTFyLkS2O|ch|ryP MXHTRW5ITVJ?
M059J M{THNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKzWY1KSzVyPUGwMlYyODJizszN NFziUYhUSU6JRWK=
HT-3 NH3jfHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFyLk[xO|kh|ryP NYrvSIZHW0GQR1XS
SNU-387 M1u2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnrendKSzVyPUGwMlczOzVizszN NFLJT2pUSU6JRWK=
NCI-H526 NF3tdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\WVppSUUN3ME2xNU4yOzZ3IN88US=> M3SwZ3NCVkeHUh?=
HEL M37Zbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjWRYpKSzVyPUGxMlY2PzlizszN MYrTRW5ITVJ?
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NCI-H2030 NFLNWHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPodJZKSzVyPUO0NU43ODlizszN NVHLNGx[W0GQR1XS
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KP-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HGbGlEPTB;M{SzMlc{OyEQvF2= NXu5OmM1W0GQR1XS
PF-382 M{D0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX65O2NTUUN3ME2zOFQvPDJ{IN88US=> NYjvW4F[W0GQR1XS
NB13 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PIOGlEPTB;M{S1MlU5KM7:TR?= NV3MbG1GW0GQR1XS
D-502MG M3XGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzRZm5mUUN3ME2zOFUvQDF{IN88US=> NILmfJVUSU6JRWK=
CAL-54 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\iPFM4UUN3ME2zOFUvQDd7IN88US=> M3jQfHNCVkeHUh?=
DOHH-2 NWno[3VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTN2Nj62OUDPxE1? M{DGVHNCVkeHUh?=
SK-PN-DW M2\jTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfG[IZTUUN3ME2zOFcvPDJ4IN88US=> MnzJV2FPT0WU
NCI-H720 NVTDZphKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXJTWM2OD1|NEmuPFQ3KM7:TR?= MVjTRW5ITVJ?
SW1990 MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvyTWM2OD1|NUGuNlgh|ryP NF7tWWtUSU6JRWK=
NCI-H2196 NIHENm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTN3Mj62NlQh|ryP M3zyR3NCVkeHUh?=
P30-OHK M{T3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HxcWlEPTB;M{WzMlA3OyEQvF2= MVPTRW5ITVJ?
NCI-H358 NYT6WI9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfVTWM2OD1|NUWuN|U3KM7:TR?= M1HGcXNCVkeHUh?=
CW-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTN3Nj61Nlkh|ryP NYrqVHB4W0GQR1XS
COLO-678 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\ZU2VJUUN3ME2zOVcvQDZ|IN88US=> NI\wWVRUSU6JRWK=
NCI-H2126 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;STWlEPTB;M{W4MlUzOSEQvF2= NFf1VYNUSU6JRWK=
DMS-53 M1fpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HlUGlEPTB;M{W4MlcyOSEQvF2= MVPTRW5ITVJ?
NCI-H1838 M3z4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7wSlBKSzVyPUO1PU46QDdizszN NGqzOI9USU6JRWK=
SJSA-1 M33DNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nCVGlEPTB;M{[wMlk{QSEQvF2= NWD1W5hyW0GQR1XS
ChaGo-K-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrvTWM2OD1|NkOuPVI1KM7:TR?= M1G2c3NCVkeHUh?=
IST-SL2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz4TWM2OD1|N{KuPVI3KM7:TR?= MUPTRW5ITVJ?
U-266 NVKxb5ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7zRZJKSzVyPUO3N{4yOzJizszN NXnwV2o3W0GQR1XS
P31-FUJ NFW3cmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTN5Nj65OlQh|ryP M2nqfHNCVkeHUh?=
HCC2157 NE\hb|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[1XHBkUUN3ME2zO|gvOTZzIN88US=> NEPkN|FUSU6JRWK=
COR-L88 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLFTWM2OD1|OEOuOlc4KM7:TR?= NIPCbYNUSU6JRWK=
NCI-H596 NInsUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULG[Zp[UUN3ME2zPFUvOzRizszN M4TSOXNCVkeHUh?=
GOTO MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Xib2lEPTB;M{mwMlY1OSEQvF2= MnHiV2FPT0WU
NCI-H719 M1fRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTN7MT64PVMh|ryP Mn7xV2FPT0WU
MN-60 MmC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN7Mz65OFgh|ryP Ml3EV2FPT0WU
IST-SL1 MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHi3W2RKSzVyPUO5OE41ODZizszN MlvUV2FPT0WU
TE-6 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P2cmlEPTB;M{m3MlI2PCEQvF2= MmDVV2FPT0WU
SW962 NXnYNYVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrwTWM2OD1|OUiuOlkh|ryP MUHTRW5ITVJ?
FADU MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e2[2lEPTB;NECzMlA5OyEQvF2= MUnTRW5ITVJ?
ECC4 MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTRyOD60OVgh|ryP NWPNOHNoW0GQR1XS
MES-SA NGPmO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIezN5ZKSzVyPUSwPU46QCEQvF2= NHzGeYFUSU6JRWK=
NCI-H716 NE\KeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rhVGlEPTB;NEGwMlA4PSEQvF2= M3;B[XNCVkeHUh?=
GR-ST NUnlZ5NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHFTWM2OD12MUCuOFk4KM7:TR?= MWLTRW5ITVJ?
KY821 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPnbXlKSzVyPUSxOE4xQDZizszN MmHpV2FPT0WU
NCI-H2141 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmxT3RKSzVyPUSyOE4{QDhizszN NEHTNGhUSU6JRWK=
MDA-MB-134-VI NHm1PW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvYTWM2OD12M{GuNFM{KM7:TR?= M3iwRXNCVkeHUh?=
RH-1 NYjyW3N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXl[G9KSzVyPUSzOU4xQSEQvF2= NX\FbGU5W0GQR1XS
AM-38 MkL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTR|OD61OEDPxE1? NGXxVIFUSU6JRWK=
BL-70 M4fCZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR|OT60Nlkh|ryP NH3hU4ZUSU6JRWK=
COLO-684 NUn3NndYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK4TWM2OD12NEiuPFg5KM7:TR?= MX7TRW5ITVJ?
DMS-79 NU\sVpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni2TWM2OD12NEmuOlgh|ryP NVnqNmNMW0GQR1XS
EW-1 M4rhOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH6[olKSzVyPUS1Nk45QDhizszN Mor6V2FPT0WU
MS-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme3TWM2OD12NUSuN|g2KM7:TR?= MWTTRW5ITVJ?
A4-Fuk M{TQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXuzUJNWUUN3ME20OVQvPTB5IN88US=> NU\yN2pHW0GQR1XS
TALL-1 NGPyZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX75NpIzUUN3ME20OVUvOjl5IN88US=> MYjTRW5ITVJ?
SCLC-21H Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTR3NT62PVkh|ryP M2fIe3NCVkeHUh?=
KMS-12-PE MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR3Nj64NlIh|ryP NF[5VHVUSU6JRWK=
TE-441-T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\HTWM2OD12NUeuNVg3KM7:TR?= M4jGdHNCVkeHUh?=
A3-KAW MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLmc5dKSzVyPUS2NE45PDFizszN M4q2dnNCVkeHUh?=
NCI-H1092 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTR4Mz65OFMh|ryP M{PzXHNCVkeHUh?=
COR-L279 NGO1OJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[yW3VKSzVyPUS2OE45PDdizszN MXHTRW5ITVJ?
NCI-SNU-5 MnXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLyTWM2OD12N{KuNlgh|ryP MmHoV2FPT0WU
JAR NHizW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr5fIxKSzVyPUS3OE44QDhizszN NYHHfnV4W0GQR1XS
NCI-H446 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETr[oJKSzVyPUS3O{4xQCEQvF2= MkO0V2FPT0WU
HDLM-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX1R4liUUN3ME20PFAvQDZ7IN88US=> MV7TRW5ITVJ?
D-283MED MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2roOmlEPTB;NEi4MlkzPCEQvF2= NGTFfZBUSU6JRWK=
NCI-H1395 NGfGOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3DbJJKSzVyPUS4PU4xODRizszN Ml\ZV2FPT0WU
RPMI-6666 MljKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTjTWM2OD12OUGuN|k5KM7:TR?= MkC3V2FPT0WU
CPC-N MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTVyMj6wOlMh|ryP M3nYbHNCVkeHUh?=
EC-GI-10 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHGySG9KSzVyPUWwNk4yPjlizszN MoPZV2FPT0WU
CA46 NU\sWFNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPh[2xKSzVyPUWwOE41ODdizszN NYXSUphJW0GQR1XS
EHEB NUPmPZdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTVyNz6yNFgh|ryP M{fzXHNCVkeHUh?=
RPMI-8402 NFfGS|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;XeWlEPTB;NUGwMlAzOSEQvF2= NUfSPXJPW0GQR1XS
DU-4475 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rXN2lEPTB;NUGxMlExOSEQvF2= MmroV2FPT0WU
P12-ICHIKAWA MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELM[o9KSzVyPUWxNU41OTZizszN NGr1TlZUSU6JRWK=
NCI-H1694 NVPzN241T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnzTWpQUUN3ME21NVIvPDN7IN88US=> MVvTRW5ITVJ?
NCI-H2171 NGmzPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojETWM2OD13MUKuO|A2KM7:TR?= MYjTRW5ITVJ?
Mo-T NWLqRYt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HLRWlEPTB;NUG1MlEyPiEQvF2= NXrNdnV{W0GQR1XS
HL-60 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DrfWlEPTB;NUKyMlkzPCEQvF2= MYPTRW5ITVJ?
NCI-H1436 NIPKXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTV{Mz6wOlQh|ryP NFjwZ5NUSU6JRWK=
NCI-H510A MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLhbHVKSzVyPUWyOE43QTZizszN Ml3xV2FPT0WU
NCI-H2081 M2LkfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITqempKSzVyPUWyOU42OTNizszN MlS0V2FPT0WU
NB5 NV7mfIpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDZeIFOUUN3ME21NlYvPDNizszN NIDz[5BUSU6JRWK=
NCI-H2227 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj0TIlKSzVyPUWzNE4zPTRizszN NHLmPJVUSU6JRWK=
HSC-4 M4rFO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTV|OT6yPVMh|ryP NUXKV4s{W0GQR1XS
RL NFjTUY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HuemlEPTB;NUSyMlQ1OiEQvF2= MVXTRW5ITVJ?
EVSA-T NIK4dpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTV2Mz62PFQh|ryP NXzSVZpmW0GQR1XS
NCI-H889 M4faTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zk[GlEPTB;NUS3MlI{KM7:TR?= NUjxT5R5W0GQR1XS
COLO-320-HSR MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu0dlZKSzVyPUW1NU4{PSEQvF2= NFu0fJVUSU6JRWK=
EW-11 M1HLUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X3PWlEPTB;NUWyMlM6QSEQvF2= NUXQb4RbW0GQR1XS
UACC-812 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm4flJ6UUN3ME21OVkvOzlzIN88US=> MmPxV2FPT0WU
CAL-148 MlfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTV4NT6wPFkh|ryP NUfoVXl[W0GQR1XS
K052 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjCTWM2OD13N{muNlE{KM7:TR?= MWHTRW5ITVJ?
L-428 M2P4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTZyMD62O|Eh|ryP M3fWcHNCVkeHUh?=
LP-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnVZ3JKSzVyPU[wN{42QDdizszN MVfTRW5ITVJ?
ML-2 NHfVXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MleyTWM2OD14ME[uOVc6KM7:TR?= M1uzTnNCVkeHUh?=
KARPAS-45 MmP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M16w[WlEPTB;NkG4MlIzOSEQvF2= MWjTRW5ITVJ?
HT NXXTXFVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG5VIxSUUN3ME22NlIvPzh3IN88US=> Mlu4V2FPT0WU
NCI-H226 NIPnVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkO3TWM2OD14MkiuN|U{KM7:TR?= M{\oU3NCVkeHUh?=
L-363 NYDV[G1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD0ZopIUUN3ME22OFgvODZ2IN88US=> M3vlPHNCVkeHUh?=
IM-9 NGWyRpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXzblBHUUN3ME22OVEvPTRzIN88US=> Mn3yV2FPT0WU
TUR Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTZ5MT6zNlIh|ryP NXrDOWJqW0GQR1XS
NCI-SNU-16 NEO5NG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTZ6MD60OlIh|ryP NETQXpRUSU6JRWK=
NCI-SNU-1 M1vVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvJc|hbUUN3ME22PVAvOTd{IN88US=> NFL2TXlUSU6JRWK=
U-87-MG M3TrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Lo[mlEPTB;Nkm0MlU5PSEQvF2= M3PFNnNCVkeHUh?=
KM-H2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLYc2JmUUN3ME22PVkvODV7IN88US=> MYnTRW5ITVJ?
DEL MoHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjjUIxKSzVyPUewNE45OzhizszN MUfTRW5ITVJ?
KARPAS-422 MnvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnoc|BRUUN3ME23PFkvOzF3IN88US=> MX3TRW5ITVJ?
BC-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPuU21KSzVyPUiwOU4zODNizszN M4nIPXNCVkeHUh?=
NCI-H1155 NGfP[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;EOWdyUUN3ME24NVgvODV7IN88US=> Mk\UV2FPT0WU
NCI-H1581 NYrPUG1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjlUohwUUN3ME25NFAvOjNzIN88US=> MX;TRW5ITVJ?

... 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]

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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]

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  • 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]

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  • 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)
Water Insoluble
Ethanol '2 mg/mL
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 Cl.CC1=C[NH]C(=N1)C2=CN=C(NCCNC3=NC=C(C=C3)C#N)N=C2C4=CC=C(Cl)C=C4Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

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

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

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

If you have any other enquiries, please leave a message.

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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