CHIR-99021 (CT99021) HCl

Catalog No.S2924

CHIR-99021 (CT99021) HCl Chemical Structure

Molecular Weight(MW): 501.8

CHIR-99021 HCl (CT99021) 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.

Size Price Stock Quantity  
In DMSO USD 340 In stock
USD 90 In stock
USD 170 In stock
USD 570 In stock
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Cited by 73 Publications

9 Customer Reviews

  • Differentiation induced by treatment with the Gsk3 inhibitor in hPSCs is β-catenin dependent. H9-7TGP cells were treated with 12 uM CH in mTeSR1 for 4 d. Immunofluorescent staining for Oct4, Isl1, and Nkx2.5 was compared with GFP expression. (Scale bars, 50 uM.)

    Proc Natl Acad Sci U S A 2012 109(27):E1848-57. CHIR-99021 (CT99021) HCl purchased from Selleck.

    Gpc4 regulates ESC response to Wnt/β-catenin signaling.  (E) Quantitative analysis of control and Gpc4-mutant beating foci exposed to the GSK3 inhibitor, CHIR 99021 (1 and 3 μM, from day 0 to day 5). Analysis was done at different time points. Gpc4- mutant cells treated with CHIR 99021 behave as controls (mean±SEM; n=2).

    Stem Cells 2012 30, 1863-1874. CHIR-99021 (CT99021) HCl purchased from Selleck.

  •  

    Characterization of rES cells. A: image of normal rES cell colonies on feeder layers. B: rES colonies were positive for AP staining. CeE: rES colonies readily expressed pluripotent markers, Sox2 (C), Oct4 (D), and SSEA-1 (E). Blue, DAPI. Scale bars: 100 um.

    J Genet Genomics 2012 39, 643e651. CHIR-99021 (CT99021) HCl purchased from Selleck.

    Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.

    J Biol Chem 2015 290(9), 5592-605 . CHIR-99021 (CT99021) HCl purchased from Selleck.

  • A. Vero cells were pretreated with the indicated concentrations of CHIR-99021 for 1 h and then infected with PEDV (MOI = 1) for 8 or 10 h. Cell lysates were prepared and analyzed using Western blotting.

    PLoS One, 2016, 11(8):e0161508. CHIR-99021 (CT99021) HCl purchased from Selleck.

     

    Smad linker phosphorylation involves GSK3 in human melanoma lines. Inhibition of Smad2 and Smad3 linker phosphorylation in the presence of the specific GSK3 specific inhibitor, CT99021. 24 hours post seeding, WM793 and 1205LU cells were serum-starved for about 16 hours, and incubated in the absence (2) or presence (+) of 2 uM of CT99021 for two hours. Immunoblots were performed as in A. p: Phosphorylated. S: Serine; T: Threonine.

    PLoS One 2012 7, e47312. CHIR-99021 (CT99021) HCl purchased from Selleck.

  • SKOV3/DDP cells were treated with a range of concentration of (A) CHIR-99021 or in combination with 20 µM cisplatin for 48 h.

    Exp Ther Med, 2016, 12(6):3851-3858. CHIR-99021 (CT99021) HCl purchased from Selleck.

     

    PANC1 cells were treated with GSK3 inhibitors SB216763 (SB 10µM or SB 20µM) or CHIR99021 (CHIR 5µM) for 72h.

    CHIR-99021 (CT99021) HCl purchased from Selleck.

  •  

     Activity of canonical WNT/ β -CATENIN signals induced by CHIR 99021 in the developing human lung. Human lung tissue explants obtained at 15 weeks of gestation were exposed to 0, 5 and 10 μM CHIR 99021 in vitro for 72 h. (A-B) Western blot analysis showed expression of β -CATENIN in human lung tissues. Results are presented as the mean ± sem of three independent experiments. *P < 0.05, **P < 0.01. (C) qRT-PCR analysis detected a dose-dependent increase in WNT signaling transcription factors and target genes following exposure to CHIR 99021. Results are presented as the mean ± sem of three independent experiments. *P < 0.05, **P < 0.01. (D-K) Histology examination showed obvious morphogenetic changes of the airway epithelial cells associated with CHIR 99021 treated lung tubes. Scale bars: D-G =100 μm; H-K = 20 μm.

    CHIR-99021 (CT99021) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description CHIR-99021 HCl (CT99021) 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.
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 NXvpcVdmTnWwY4Tpc44hSXO|YYm= NXTRPVNzOyEQvF2= MljWOEBp MWnEUXNQ NIDsfpdKdmirYnn0d{BxemWjZHnwc4N6fGViZHnm[oVz\W62aXH0bY9v M1jtblEzODV3MkCw
insulin receptor–expressing CHO-IR Mnu1SpVv[3Srb36gRZN{[Xl? MmnWOVAxKG6P NFHtXVE{OCCvaX6= NGX3TXpFVVOR MYjBZ5RqfmG2ZYOgS4x6[2:pZX6gV5lvfGijc3WgLGdUMQ>? NGnW[2IyOjZyNkS5Oy=>
H4IIE MnLkSpVv[3Srb36gRZN{[Xl? NG\YRW0yOCEQvF2= NV\XXIdTOjRiaB?= NHe5VnFFVVOR MYHS[Yd2dGG2ZYOg{tIu[2G2ZX7pckBi[3Srdnn0fUBidmRiVFnSSUBkd262YXnubY5oKHC{b33veIVzKGGldHn2bZR6 MoTzNVU{PTBzOUW=
Oct4/Sox2/Klf4-infected MEFs NGLtUHpHfW6ldHnvckBCe3OjeR?= MmjMNVAh|ryP MVmyPEBl MWnEUXNQ NXftNHlNWHKxbX;0[ZMhVUWIczDy[ZBzd2e{YX3tbY5oKFS{YX7z[JVk\WRiYomgU4N1PCxiU3;4Nkwh[W6mIFvs[lQ> NYrIUoZHOTl6M{mwOVU>
Sca-1+ HPC M2TlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLVNkDPxE1? MmLFOkBl NUP2SFNSTE2VTx?= MkLpV5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NYf3NXZNOjF4MkSzOFg>
HMC1.2 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYSxdGd4OzBizszN MmnPO|IhcA>? MVXEUXNQ Mn31VoVlfWOnczDj[YxtKHO3co\peoFt M{XMb|IzODN7M{Cx
Endothelial cell(EC) M4[3XWZ2dmO2aX;uJGF{e2G7 MYGzJO69VQ>? NHnOO|NFVVOR MV;Qdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u Mn7TNlIxPTJyME[=
PANC1 NVuzb5RoSXCxcITvd4l{KEG|c3H5 MmfGxsA2KM7:TR?= NFv4T|Q4OiCq MV;EUXNQ NWPxTXFbXHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn MUWyNlIxOTF6Nh?=
INS-1E M1rkTWZ2dmO2aX;uJGF{e2G7 M2PUWFIvPSEQvF2= NUHZRWRqOjRiaB?= NGW0UZpFVVOR NWrxS|R6UW6mdXPld{BiKHKnZIXjeIlwdiCxZjDOVFEhd3[ncnX4dJJme3Orb36= NEnTW3AzOjR{N{ewOC=>
hiPSC-NPs M4nYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTG[GZNO+LCid88US=> Ml\rO|IhcA>? M3HWbGROW09? MknuTY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh MoLvNlI3PDJ4OEe=
platelets NEe2cpZHfW6ldHnvckBCe3OjeR?= MkLGNVAh|ryP M{OzVVE2KG2rbh?= M4XtTmROW09? M3mzPGlv[3KnYYPld{B1cHKxbXLpck1u\WSrYYTl[EBxdGG2ZXzleEBi\2e{ZXfheIlwdiCjbnSgRXRRKHOnY4LleIlwdg>? NXf6cJloOjN{M{m4O|c>
DN3 NGXySWRHfW6ldHnvckBCe3OjeR?= M1;0bFExKM7:TR?= NXu5dXBFQTZiaB?= M3TWZmROW09? NVniN5BQUW6lcnXhd4V{KGOnbHyg[IV3\WyxcH3lcpQh[W6mIIDyc4xq\mW{YYTpc44> M37jcFI{PTJ4OUi5
embryonic stem cells (ESC) M2DoWWZ2dmO2aX;uJGF{e2G7 NVnRVXV3OyEEtV2= NIrNPW8yOSCm M1rTUWROW09? M4fVV3Bzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= MV:yN|g1OzNzMh?=
H460 NIHJbldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrsOlA2KML3TR?= M1rnTlI1KGh? MX\EUXNQ MVHQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= MljoNlQ{Pjd4OEi=
H157 NIf2N2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFewVIs2KML3TR?= M13aTlI1KGh? MULEUXNQ MoTiVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u NGCyfZAzPDN4N{[4PC=>
H460 NFGybpVCeG:ydH;zbZMhSXO|YYm= MlXTOUDDvU1? NGPVRogzPCCq NFrOT|dFVVOR NVewR|RbSXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> NEDrWIQzPDN4N{[4PC=>
H157 M17IZ2Fxd3C2b4Ppd{BCe3OjeR?= NXyySFhtPSEEtV2= MXmyOEBp MoL0SG1UVw>? MYTEc4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> NGW5V|UzPDN4N{[4PC=>
A549 MX\BdI9xfG:|aYOgRZN{[Xl? M{DsZlUhyrWP NH;6T20zPCCq MmjFSG1UVw>? NFrqNWxKdmO{ZXHz[ZMh[2WubDDhdI9xfG:|aYO= MmXCNlQ{Pjd4OEi=
Neural progenitor cells M3;NWWZ2dmO2aX;uJGF{e2G7 NEX2WIs{KM7:TR?= MWmxNEBl M{XNW2ROW09? MVHJcoR2[2W|IHflcoVz[XSrb36gc4YhdmW3cnHsJJBzd2enbnn0c5Ih[2WubIO= M2fydVI1PjN6MEO0
ES-D3 M3K3eGN6fG:2b4jpZ{BCe3OjeR?= MXKxNOKh|ryP MYCzJIQ> MlexSG1UVw>? M3HhSWlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP NVHnTW82OjR5N{mzOlU>
ES-CCE NEXndJhEgXSxdH;4bYMhSXO|YYm= MofzNVDDqM7:TR?= M4DGflMh\A>? MnvXSG1UVw>? NIfGeXdKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? NUfBbJRPOjR5N{mzOlU>
ES-D3 MmDJSpVv[3Srb36gRZN{[Xl? MVy1xsDPxE1? MU[zJIQ> MnT5SG1UVw>? NX;ZN3k3W3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 MUCyOFc4QTN4NR?=
ES-CCE M1rhUmZ2dmO2aX;uJGF{e2G7 NV62N2J2PcLizszN NV\jSnhHOyCm NFfIRVRFVVOR M33WPHN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? MVGyOFc4QTN4NR?=
SW982 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\W[mlEPTB;MD6yNVQyPiEQvF2= MUHTRW5ITVJ?
GCT NITsVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zTOmlEPTB;MD6zNFY4OiEQvF2= NFTHNJJUSU6JRWK=
769-P M{jsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\neGhNUUN3ME2wMlU5PDl7IN88US=> NIjzdXFUSU6JRWK=
LOXIMVI NHTyU5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLpTWM2OD1yLkW4PFMzKM7:TR?= MVHTRW5ITVJ?
D-336MG MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfybWVKSzVyPUCuPFQ3OiEQvF2= MYjTRW5ITVJ?
S-117 NIX5XYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwOUKxN|Eh|ryP NGfyco5USU6JRWK=
D-247MG MnHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPRT41jUUN3ME2wMlk1QDV{IN88US=> MnvHV2FPT0WU
TYK-nu NXnmRoV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrCT4lKSzVyPUGuNFc6OTJizszN MoG4V2FPT0WU
A498 M3X0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DsWGlEPTB;MT6zNFQ3QSEQvF2= NXLHR5k2W0GQR1XS
BCPAP NIDiTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jpVGlEPTB;MT62Olg6QCEQvF2= MWLTRW5ITVJ?
KYSE-180 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTFwN{K3PFgh|ryP M134RXNCVkeHUh?=
MIA-PaCa-2 NFS2fZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDUPWhEUUN3ME2xMlc2QTd5IN88US=> NFrUU|RUSU6JRWK=
HCC1395 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwN{iyO|Mh|ryP NGi3[I1USU6JRWK=
RS4-11 NUfxbW5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ZTWM2OD1zLkm1OFE2KM7:TR?= MVTTRW5ITVJ?
NCI-H2122 NI\DWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zYfWlEPTB;Mj6yO|Y5PCEQvF2= NFe4cJRUSU6JRWK=
SNU-423 NGrOcXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvZd4FKSzVyPUKuOFk4QDdizszN MVLTRW5ITVJ?
SK-LMS-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnY[FY2UUN3ME2yMlY1OTJ6IN88US=> MnHpV2FPT0WU
RPMI-7951 M2m2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrpTWM2OD1{LkewNVk{KM7:TR?= NITISGNUSU6JRWK=
COLO-829 NGm5ZmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfrTWM2OD1{Lke2OVQh|ryP NFXpNlFUSU6JRWK=
SCC-9 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LrT2lEPTB;Mj65OVQ5PSEQvF2= M1;wN3NCVkeHUh?=
A704 NGjFb3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfiTWM2OD1|LkC4NVIh|ryP MX7TRW5ITVJ?
HOP-62 NFPHeWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPZTXdMUUN3ME2zMlM3ODV2IN88US=> M3f4NXNCVkeHUh?=
HCC1569 NX;TUGRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzqdmk{UUN3ME2zMlQ5OzB3IN88US=> Mk\rV2FPT0WU
A172 M{jFWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TncmlEPTB;Mz63OVQ6QCEQvF2= M4jlWnNCVkeHUh?=
MOLT-16 NIH0XJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:5e5l[UUN3ME2zMlg5PTV4IN88US=> M3\rOHNCVkeHUh?=
TE-15 M1\UdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LV[2lEPTB;Mz65OVM1OyEQvF2= NHvXO4pUSU6JRWK=
OE19 MnjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTpOZBKSzVyPUOuPVY1PTFizszN M3yy[nNCVkeHUh?=
MHH-ES-1 MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP6TWM2OD12LkC0OVQ2KM7:TR?= MWLTRW5ITVJ?
NKM-1 NIPvcWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7WTWM2OD12LkGzPVcyKM7:TR?= MlLZV2FPT0WU
RCC10RGB M1flSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrNTWM2OD12LkK5OFc6KM7:TR?= Mk\XV2FPT0WU
BxPC-3 M{Dkbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTRwN{CzPVEh|ryP NXix[5YzW0GQR1XS
ALL-PO NWns[JE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTRwOEO4OVgh|ryP MV7TRW5ITVJ?
SK-OV-3 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTRwOUmzOEDPxE1? MoHUV2FPT0WU
SW1710 NHXEOndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTVwNEK0OVYh|ryP MXHTRW5ITVJ?
NCI-H2452 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M32wOGlEPTB;NT60OVYzQCEQvF2= MUTTRW5ITVJ?
D-392MG NHO2[oJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPCOWJKSzVyPUWuOFkyPDVizszN MYfTRW5ITVJ?
LB2518-MEL M3XPUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH62blBKSzVyPUWuO|I3OjdizszN NYnjT2ZuW0GQR1XS
BL-41 NYfxPFdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M32xR2lEPTB;NT64NVI3PiEQvF2= NVHyTHBzW0GQR1XS
WM-115 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq1T4VuUUN3ME21MlgyPTB7IN88US=> MkX0V2FPT0WU
SK-MEL-2 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTHd3JKSzVyPU[uN|g{PDRizszN NHjFTmNUSU6JRWK=
CGTH-W-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2myOGlEPTB;Nj60NVch|ryP MmTXV2FPT0WU
BB65-RCC MljBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fvSWlEPTB;Nj61N|E6PSEQvF2= MoexV2FPT0WU
CAL-85-1 MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTZwNkC5N|Yh|ryP M4LTbnNCVkeHUh?=
RT-112 NWLo[5Q3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi4d5pTUUN3ME23MlE3PDV4IN88US=> NUG1cmpVW0GQR1XS
MC116 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF24UFNKSzVyPUeuNlg3QTFizszN M1XDTHNCVkeHUh?=
G-361 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTMTWM2OD15LkS2OVYyKM7:TR?= NH[4S4RUSU6JRWK=
SW1417 NVLI[JN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrTXIJXUUN3ME23MlY1PTh2IN88US=> NEnpToNUSU6JRWK=
MV-4-11 NVXuVGpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT5d2Y6UUN3ME24MlU1OzB2IN88US=> NY\oUoE5W0GQR1XS
CAL-72 M4PBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH21UIZKSzVyPUiuO|YyOTNizszN MUDTRW5ITVJ?
MKN28 NF7Td21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XiOWlEPTB;OD64PFUyPiEQvF2= NGXiPWFUSU6JRWK=
MEG-01 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S3[mlEPTB;OD65PVA1OyEQvF2= M3n4NXNCVkeHUh?=
ACHN M1X1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknNTWM2OD17LkOwOVQ3KM7:TR?= MnnwV2FPT0WU
NCI-H1755 NWXOWHdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[3No52UUN3ME25MlM6QTh4IN88US=> NYPMNJNmW0GQR1XS
NCI-H64 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPZTWM2OD17LkSyNlU2KM7:TR?= MlrRV2FPT0WU
COLO-205 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rPVGlEPTB;OT60N|gzOSEQvF2= NYfuWlJHW0GQR1XS
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U-2-OS NW\OR2xNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX6wZpR[UUN3ME25MlQ2ODB4IN88US=> NG\N[IRUSU6JRWK=
LB996-RCC NUjEcVhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH1c25KSzVyPUmuOVI{QTdizszN M4\KXXNCVkeHUh?=
SK-N-DZ MkXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTlwNkW3OFIh|ryP MVvTRW5ITVJ?
EFM-19 NHG1OYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv5V4M{UUN3ME25Mlc2PTZ4IN88US=> NUL4OFJpW0GQR1XS
DBTRG-05MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DSNWlEPTB;OT63O|c4KM7:TR?= MmTiV2FPT0WU
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LB1047-RCC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTlwOUm3PVgh|ryP M4i0bnNCVkeHUh?=
NCI-H28 NFrEV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLjNFhKSzVyPUGwMlQ1OTNizszN MWHTRW5ITVJ?
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M059J NGLGTGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFyLk[xNFIh|ryP M2PMOHNCVkeHUh?=
HT-3 NIfNOFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LQR2lEPTB;MUCuOlE4QSEQvF2= M2HJdXNCVkeHUh?=
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NCI-H526 NFLUdlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2izSmlEPTB;MUGuNVM3PSEQvF2= NGXRPFRUSU6JRWK=
HEL Mlu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnG3TWM2OD1zMT62OVc6KM7:TR?= M3nnT3NCVkeHUh?=
PA-1 MlHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOwUVJKSzVyPUGxMlk{KM7:TR?= NIXGdpdUSU6JRWK=
PC-14 NEGxUFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q0WGlEPTB;MUKuN|I1KM7:TR?= NFjxRYhUSU6JRWK=
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NCI-H82 Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF|LkK5NFkh|ryP NFT6O3pUSU6JRWK=
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T98G MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFy5SVNKSzVyPUGzMlQ4OTdizszN NXPCNWsyW0GQR1XS
KU812 NGj6[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnNXWE2UUN3ME2xN{42OTd3IN88US=> MoTiV2FPT0WU
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NB1 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXzWGpGUUN3ME2xOE4yQTN3IN88US=> MUHTRW5ITVJ?
ST486 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTF2LkKyOVEh|ryP NV7Hem01W0GQR1XS
LoVo NVfOWnBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF3LkK2OVkh|ryP MUXTRW5ITVJ?
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Daudi MkPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjqOJpKSzVyPUG3MlYyPDlizszN NYnrRVV2W0GQR1XS
SIMA NXuxelZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL3WphjUUN3ME2xO{46OTF6IN88US=> NGW1VHBUSU6JRWK=
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Becker NFnPS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[2So1mUUN3ME2yNE4yPzd5IN88US=> MofiV2FPT0WU
NCI-H727 MkDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPWTWM2OD1{MD6yNVY6KM7:TR?= NE\sW4JUSU6JRWK=
HCC1187 NWDCVXcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrG[HJTUUN3ME2yNE4{PTh7IN88US=> NX3WdVgxW0GQR1XS
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EoL-1- MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\i[WlEPTB;MkGuPFM5PSEQvF2= NX;GZ4d7W0GQR1XS
TGBC24TKB MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLGTWM2OD1{MT64PVU4KM7:TR?= MWPTRW5ITVJ?
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LS-513 M3jpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJ{Lk[xPVIh|ryP M4HDd3NCVkeHUh?=
KURAMOCHI NVyzZYNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJ{LkewOlkh|ryP MXrTRW5ITVJ?
GI-1 MmDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrDWHUyUUN3ME2yNk44QDRzIN88US=> Mn2yV2FPT0WU
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PANC-10-05 NHj4bVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjOcGNDUUN3ME2yOE4xQDl6IN88US=> NYDsS4FIW0GQR1XS
HMV-II MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fJ[2lEPTB;MkSuNlE3OyEQvF2= MV;TRW5ITVJ?
NCI-H1963 NFHCV2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSyUVF4UUN3ME2yOE4zQDN7IN88US=> NHu3VnpUSU6JRWK=
LU-139 NIXVcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTJ2LkizOUDPxE1? NUDUWmZIW0GQR1XS
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RO82-W-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrNTWM2OD1{Nj63N|c4KM7:TR?= NHjKOJhUSU6JRWK=
NCI-H1770 NYPoNopYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvzTVNwUUN3ME2yOk45QTh4IN88US=> NF60[ZRUSU6JRWK=
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KLE Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDEN|diUUN3ME2yO{4zPTZ3IN88US=> Mn7HV2FPT0WU
NCI-H2170 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTJ5LkWyPFIh|ryP NF7STGlUSU6JRWK=
COLO-792 Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnJVY1qUUN3ME2yO{44PzJ6IN88US=> M3P6RnNCVkeHUh?=
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OAW-28 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjXTWM2OD1{OD6wNFUzKM7:TR?= Mm[zV2FPT0WU
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SW872 NYW3dFdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHyTWM2OD1{OD61N|I3KM7:TR?= MnXHV2FPT0WU
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LCLC-103H M3T4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{e4N2lEPTB;M{CuNlA2QSEQvF2= NFv3WVdUSU6JRWK=
CAKI-1 NG\XWVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfIfItCUUN3ME2zNE4zPjV4IN88US=> NVzFO3ZtW0GQR1XS
NALM-6 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C0WWlEPTB;M{CuOFk3PSEQvF2= MUnTRW5ITVJ?
SK-MM-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\2TWM2OD1|MD65O|kzKM7:TR?= M3rlUXNCVkeHUh?=
LB373-MEL-D NUD5UnlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HqemlEPTB;M{GuNFA1PyEQvF2= NHjF[3RUSU6JRWK=
CAS-1 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HCdWlEPTB;M{GuO|Y3PSEQvF2= M1XYXnNCVkeHUh?=
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NCI-H1648 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vDcGlEPTB;M{KuPFQ3PyEQvF2= MlXOV2FPT0WU
RVH-421 NVTiTGE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jKdWlEPTB;M{OuNVY5KM7:TR?= NFHF[25USU6JRWK=
KU-19-19 NETTd2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWq4RYNQUUN3ME2zN{44PTN2IN88US=> M3;VSXNCVkeHUh?=
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MPP-89 M{PjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrKTWM2OD12MT65NlEyKM7:TR?= Mm\hV2FPT0WU
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KYSE-270 M4[xfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[wTWM2OD12NT6wOFM4KM7:TR?= MorBV2FPT0WU
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UACC-62 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HWSWlEPTB;NE[uPFYxQCEQvF2= NHvnUXZUSU6JRWK=
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NCI-H747 M{KwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTR5LkeyOlQh|ryP MoS1V2FPT0WU
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COR-L105 NGrXXW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jzVmlEPTB;NEiuPVc{KM7:TR?= NXzEeGhnW0GQR1XS
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LC4-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvqTWM2OD12OT64PVEzKM7:TR?= MUjTRW5ITVJ?
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... Click to View More Cell Line Experimental Data

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:

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  • Animal Models: Female db/db mice or male ZDF rats with type 2 diabetes
  • Formulation: Formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.
  • 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

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
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    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.

GSK-3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID