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.

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In DMSO USD 340 In stock
USD 90 In stock
USD 170 In stock
USD 570 In stock

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Cited by 70 Publications

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  • 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.

  • 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.

     

    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.

  •  

    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.

     

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
Tie-2 [1]
(Cell-free assay)
FLT1 [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
6.7 nM 10 nM >5 μM >5 μM >5 μM
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 NEjWe2dHfW6ldHnvckBCe3OjeR?= M3;rOlMh|ryP NELTXXU1KGh? NHvLcWNFVVOR MV7Jcohq[mm2czDwdoVi\Gmyb3P5eIUh\GmoZnXy[Y51cWG2aX;u MYCxNlA2PTJyMB?=
insulin receptor–expressing CHO-IR M2jwN2Z2dmO2aX;uJGF{e2G7 NWTvTlJyPTByIH7N MkLsN|AhdWmw NWWwXIVETE2VTx?= NX;WRVlVSWO2aY\heIV{KEeueXPv[4VvKFO7boToZZNmKCiJUzm= NXe1V3NxOTJ4ME[0PVc>
H4IIE NFLpTINHfW6ldHnvckBCe3OjeR?= MmjuNVAh|ryP MWiyOEBp Mn[wSG1UVw>? M3W5U3Jm\3WuYYTld{DPui2lYYTlcolvKGGldHn2bZR6KGGwZDDUTXJGKGOxboThbY5qdmdicILvcY91\XJiYXP0bZZqfHl? MYexOVM2ODF7NR?=
Oct4/Sox2/Klf4-infected MEFs NXGx[I1RTnWwY4Tpc44hSXO|YYm= NFvO[XQyOCEQvF2= M2XzNFI5KGR? M2DwRWROW09? NYrFTZlVWHKxbX;0[ZMhVUWIczDy[ZBzd2e{YX3tbY5oKFS{YX7z[JVk\WRiYomgU4N1PCxiU3;4Nkwh[W6mIFvs[lQ> NF7rU4MyQTh|OUC1OS=>
Sca-1+ HPC NFi2d|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPNNkDPxE1? MYq2JIQ> M3XmemROW09? NEXEUYVUgW6ncnfpd5Rq[2GubImgdJJwdW:2ZYOgV4NiNTFtwrDIVGMheHKxbHnm[ZJifGmxbjDhcoQh[2:ub375JIZwem2jdHnvckB1d2endHjldkB4cXSqIFXHSi=> NUjxSHN{OjF4MkSzOFg>
HMC1.2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmzNEDPxE1? MWW3NkBp M1myXWROW09? M2q5ZXJm\HWlZYOgZ4VtdCC|dYL2bZZidA>? NVHQZ3FuOjJyM{mzNFE>
Endothelial cell(EC) MmezSpVv[3Srb36gRZN{[Xl? NF3kSIM{KM7:TR?= MX3EUXNQ MUPQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u MoTINlIxPTJyME[=
PANC1 MV3BdI9xfG:|aYOgRZN{[Xl? MWJCpFUh|ryP NEnqUFM4OiCq NEWxSIdFVVOR MYnUdolo\2W{czDhckBieG:ydH;0bYMhemW|cH;ud4U> M3L0c|IzOjBzMUi2
INS-1E NETpe3lHfW6ldHnvckBCe3OjeR?= NF7tfoIzNjVizszN M1fHWlI1KGh? Mn:3SG1UVw>? NYDabYZNUW6mdXPld{BiKHKnZIXjeIlwdiCxZjDOVFEhd3[ncnX4dJJme3Orb36= NWrWRmpCOjJ2Mke3NFQ>
hiPSC-NPs M13VVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmz5qCK|ryP MU[3NkBp NUX6PHQ2TE2VTx?= NEH6S3pKdmO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vyqB? MontNlI3PDJ4OEe=
platelets M4nuVGZ2dmO2aX;uJGF{e2G7 NWPJVmUzOTBizszN MV2xOUBucW5? Ml;XSG1UVw>? NH\yb4FKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? MUOyN|I{QTh5Nx?=
DN3 NX3YUYpPTnWwY4Tpc44hSXO|YYm= MVKxNEDPxE1? M3;LeVk3KGh? NVPCNmdJTE2VTx?= NGDP[pJKdmO{ZXHz[ZMh[2WubDDk[ZZmdG:ybXXueEBidmRicILvcIln\XKjdHnvci=> M1i3WFI{PTJ4OUi5
embryonic stem cells (ESC) M1PHbWZ2dmO2aX;uJGF{e2G7 MVizJOK2VQ>? MXuxNUBl M3fUbWROW09? MorFVJJwdW:2ZYOgd4Vt\i2{ZX7le4FtKG:oIH7hx893\S22eYDlJI1wfXOnIHXtZpJ6d26rYzDzeIVuKGOnbHzzJEhGW0Nr M1PqTFI{QDR|M{Gy
H460 M{f4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn6[JB7PSEEtV2= NH;ofJUzPCCq NIrFVphFVVOR M3i1SXBzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> MVeyOFM3PzZ6OB?=
H157 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW4OUDDvU1? MnjyNlQhcA>? MnnFSG1UVw>? NWnqU|BJWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v NVnNNnoyOjR|Nke2PFg>
H460 MlntRZBweHSxc3nzJGF{e2G7 NEf2OmY2KML3TR?= MoTWNlQhcA>? MVnEUXNQ M4LZNWF1fGWwdXH0[ZMh[2WubDDhdI9xfG:|aYO= M2D4cFI1OzZ5Nki4
H157 NVuwRZh7SXCxcITvd4l{KEG|c3H5 NVHyTol5PSEEtV2= M{W5ZVI1KGh? NGXWU|NFVVOR NVrReHp3TG:nczDuc5Qhe2mpbnnmbYNidnSueTDh[oZm[3RiYYDvdJRwe2m| MUKyOFM3PzZ6OB?=
A549 NEP2dpNCeG:ydH;zbZMhSXO|YYm= M{XNN|UhyrWP MlW2NlQhcA>? MWnEUXNQ M2nIPWlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= Mm[2NlQ{Pjd4OEi=
Neural progenitor cells NFfIV5RHfW6ldHnvckBCe3OjeR?= Mmn4N{DPxE1? Mkn5NVAh\A>? M{L1NGROW09? MX3JcoR2[2W|IHflcoVz[XSrb36gc4YhdmW3cnHsJJBzd2enbnn0c5Ih[2WubIO= MWiyOFY{QDB|NB?=
ES-D3 NGTNWnJEgXSxdH;4bYMhSXO|YYm= NIDuVIoyOMLizszN NV3DT4p2OyCm NUC5em1jTE2VTx?= NITGZ3RKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gSC5aYToJGlEPTBib3[gOE46KM7:TR?= MUWyOFc4QTN4NR?=
ES-CCE NX\BTmJKS3m2b4TvfIlkKEG|c3H5 NYThcHBOOTEEoN88US=> NV7OTmE3OyCm NYS1e3ZITE2VTx?= MlfZTY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJk> MXWyOFc4QTN4NR?=
ES-D3 NGPzO|JHfW6ldHnvckBCe3OjeR?= MlLTOeKh|ryP NH[5dHc{KGR? MXrEUXNQ MYPTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> Mk\uNlQ4Pzl|NkW=
ES-CCE NU\nSGRrTnWwY4Tpc44hSXO|YYm= NUftS3pbPcLizszN MYCzJIQ> Mn7rSG1UVw>? MXXTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> M1fURVI1Pzd7M{[1
SW982 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\GWWNKSzVyPUCuNlE1OTZizszN NIjaZYRUSU6JRWK=
GCT NUfHR2dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7ONXFKSzVyPUCuN|A3PzJizszN MXPTRW5ITVJ?
769-P MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwNUi0PVkh|ryP M1GzR3NCVkeHUh?=
LOXIMVI NGH3NW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TkbGlEPTB;MD61PFg{OiEQvF2= M1\SSHNCVkeHUh?=
D-336MG NEmycHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P2bWlEPTB;MD64OFYzKM7:TR?= MkH1V2FPT0WU
S-117 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwOUKxN|Eh|ryP MoTlV2FPT0WU
D-247MG MkHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGye3VKSzVyPUCuPVQ5PTJizszN M{jCenNCVkeHUh?=
TYK-nu NIfDO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofmTWM2OD1zLkC3PVEzKM7:TR?= NIXSZVdUSU6JRWK=
A498 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjRblJJUUN3ME2xMlMxPDZ7IN88US=> NXnGOlRnW0GQR1XS
BCPAP MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwNk[4PVgh|ryP NVSxdVlsW0GQR1XS
KYSE-180 NUfCeY1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFwN{K3PFgh|ryP NYPJZ2g2W0GQR1XS
MIA-PaCa-2 NVXP[olNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDYTWM2OD1zLke1PVc4KM7:TR?= NYfSO5REW0GQR1XS
HCC1395 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPiXnhwUUN3ME2xMlc5Ojd|IN88US=> MVTTRW5ITVJ?
RS4-11 M{nyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi4bpRKSzVyPUGuPVU1OTVizszN NGrMNIJUSU6JRWK=
NCI-H2122 MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe0VII2UUN3ME2yMlI4Pjh2IN88US=> NVjsTXUyW0GQR1XS
SNU-423 M{LxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3DTWM2OD1{LkS5O|g4KM7:TR?= M{POXXNCVkeHUh?=
SK-LMS-1 M{HMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DOS2lEPTB;Mj62OFEzQCEQvF2= MYfTRW5ITVJ?
RPMI-7951 MmryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DtZ2lEPTB;Mj63NFE6OyEQvF2= MYPTRW5ITVJ?
COLO-829 M1[yVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJwN{[1OEDPxE1? M2HnUXNCVkeHUh?=
SCC-9 NWTmXWo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzyTWM2OD1{Lkm1OFg2KM7:TR?= MlXsV2FPT0WU
A704 NILTVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTNwMEixNkDPxE1? NVP1PWhQW0GQR1XS
HOP-62 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn5eJNKSzVyPUOuN|YxPTRizszN M2jiRXNCVkeHUh?=
HCC1569 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHuU2dEUUN3ME2zMlQ5OzB3IN88US=> NHTjZ5JUSU6JRWK=
A172 MmfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTNwN{W0PVgh|ryP MWrTRW5ITVJ?
MOLT-16 NITjSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPsTWM2OD1|Lki4OVU3KM7:TR?= MlHKV2FPT0WU
TE-15 NYDYV2xCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNwOUWzOFMh|ryP MmPaV2FPT0WU
OE19 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\zOYxKSzVyPUOuPVY1PTFizszN NHHQd|FUSU6JRWK=
MHH-ES-1 NIjLVJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjQTWM2OD12LkC0OVQ2KM7:TR?= Mn3xV2FPT0WU
NKM-1 NX3CfYt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPnWnVTUUN3ME20MlE{QTdzIN88US=> NIHrdW9USU6JRWK=
RCC10RGB MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjxO3pKSzVyPUSuNlk1PzlizszN NUTUeJlOW0GQR1XS
BxPC-3 M4rZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj3TWM2OD12LkewN|kyKM7:TR?= Mk\JV2FPT0WU
ALL-PO NIPPOIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoizTWM2OD12LkizPFU5KM7:TR?= Mn[zV2FPT0WU
SK-OV-3 MorVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHWTWM2OD12Lkm5N|Qh|ryP MmXGV2FPT0WU
SW1710 M17zfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTVwNEK0OVYh|ryP NF;1UnJUSU6JRWK=
NCI-H2452 M2H0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPKTWM2OD13LkS1OlI5KM7:TR?= MV;TRW5ITVJ?
D-392MG NXfxcGJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[5eGlEPTB;NT60PVE1PSEQvF2= NUDwd2tUW0GQR1XS
LB2518-MEL NWnvd2pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\jTWM2OD13LkeyOlI4KM7:TR?= MlPPV2FPT0WU
BL-41 NIK5VotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfZeVNPUUN3ME21MlgyOjZ4IN88US=> MmiwV2FPT0WU
WM-115 NXzsbJVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHjTWM2OD13LkixOVA6KM7:TR?= MXHTRW5ITVJ?
SK-MEL-2 M3S2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTZwM{izOFQh|ryP NGrYToZUSU6JRWK=
CGTH-W-1 NG\sRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj0cWhxUUN3ME22MlQyPyEQvF2= M4LZZXNCVkeHUh?=
BB65-RCC NXX1d3lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnncmlKSzVyPU[uOVMyQTVizszN MUPTRW5ITVJ?
CAL-85-1 MlH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIq5RZBKSzVyPU[uOlA6OzZizszN NFfKRWNUSU6JRWK=
RT-112 NETVTWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jCTGlEPTB;Nz6xOlQ2PiEQvF2= NXfk[VdxW0GQR1XS
MC116 M3jKdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;TTWM2OD15LkK4OlkyKM7:TR?= NUHve|hyW0GQR1XS
G-361 NEfpUWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3nTWM2OD15LkS2OVYyKM7:TR?= NGLLSJFUSU6JRWK=
SW1417 NXHJOlRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULvOmNkUUN3ME23MlY1PTh2IN88US=> NVOyWZVrW0GQR1XS
MV-4-11 NGnhWGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRThwNUSzNFQh|ryP Mnu3V2FPT0WU
CAL-72 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zTNmlEPTB;OD63OlEyOyEQvF2= MVjTRW5ITVJ?
MKN28 NHflcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXjbIRtUUN3ME24Mlg5PTF4IN88US=> M4HLU3NCVkeHUh?=
MEG-01 NIryUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRThwOUmwOFMh|ryP NUPKe4R4W0GQR1XS
ACHN NGKyNJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTlwM{C1OFYh|ryP MULTRW5ITVJ?
NCI-H1755 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17mc2lEPTB;OT6zPVk5PiEQvF2= M2q3OHNCVkeHUh?=
NCI-H64 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\ETWM2OD17LkSyNlU2KM7:TR?= Ml34V2FPT0WU
COLO-205 MoWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTZTWM2OD17LkSzPFIyKM7:TR?= NHjrSJFUSU6JRWK=
CTV-1 NEnSPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGCyNJRKSzVyPUmuOFM5QTRizszN MX\TRW5ITVJ?
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Daudi NEfhfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e4NWlEPTB;MUeuOlE1QSEQvF2= NYDz[YRrW0GQR1XS
SIMA NVHycItFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUewdJk3UUN3ME2xO{46OTF6IN88US=> M162NnNCVkeHUh?=
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RXF393 Mo\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLGTWM2OD1{Mj62NFY5KM7:TR?= MlzyV2FPT0WU
LS-513 M3;LdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrSTHdHUUN3ME2yNk43OTl{IN88US=> MUXTRW5ITVJ?
KURAMOCHI MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ja[GlEPTB;MkKuO|A3QSEQvF2= MlTYV2FPT0WU
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M14 NEPDZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3UNnd7UUN3ME2yN{4yOTN{IN88US=> NXrse444W0GQR1XS
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PANC-10-05 Ml3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jSO2lEPTB;MkSuNFg6QCEQvF2= NIfZSFZUSU6JRWK=
HMV-II MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O3bGlEPTB;MkSuNlE3OyEQvF2= NVjRO5ZDW0GQR1XS
NCI-H1963 NUTlNI45T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnTTWZHUUN3ME2yOE4zQDN7IN88US=> M4OxOnNCVkeHUh?=
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NCI-H1770 MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorTTWM2OD1{Nj64PVg3KM7:TR?= M{G5VnNCVkeHUh?=
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KLE NHG2c4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\h[GNwUUN3ME2yO{4zPTZ3IN88US=> NUjtS4UyW0GQR1XS
NCI-H2170 NV7Re4lQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\H[HRIUUN3ME2yO{42Ojh{IN88US=> MoPVV2FPT0WU
COLO-792 NVLnd5lOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\MO3BNUUN3ME2yO{44PzJ6IN88US=> MnnHV2FPT0WU
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JiyoyeP-2003 NUHHUIo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;QVWlIUUN3ME2yPU43PzF7IN88US=> MoLYV2FPT0WU
A204 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ7Lk[4Nlgh|ryP MYjTRW5ITVJ?
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LCLC-103H MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LwZ2lEPTB;M{CuNlA2QSEQvF2= MUTTRW5ITVJ?
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SK-MM-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTNyLkm3PVIh|ryP M3\oOXNCVkeHUh?=
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CAS-1 NW\TN3UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXJS2ROUUN3ME2zNU44PjZ3IN88US=> MWDTRW5ITVJ?
KNS-42 M1zZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK4coR7UUN3ME2zNU45PjZ{IN88US=> NV\Z[4liW0GQR1XS
SW948 Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[0c3NiUUN3ME2zNk44PTR6IN88US=> M4X5THNCVkeHUh?=
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NCI-H1648 NFqzOItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmCxTWM2OD1|Mj64OFY4KM7:TR?= M{TMOXNCVkeHUh?=
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HT-144 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTN6LkK1O|Uh|ryP MWHTRW5ITVJ?
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HT M3vPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vJWWlEPTB;NkKyMlc5PSEQvF2= NVzjVZNTW0GQR1XS
NCI-H226 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\NRnNmUUN3ME22NlgvOzV|IN88US=> MnjMV2FPT0WU
L-363 M4rxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTZ2OD6wOlQh|ryP NEGwNndUSU6JRWK=
IM-9 MoO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTZ3MT61OFEh|ryP Mm\QV2FPT0WU
TUR MmHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmm4TWM2OD14N{GuN|IzKM7:TR?= NH24TllUSU6JRWK=
NCI-SNU-16 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTZ6MD60OlIh|ryP NXjtWVQzW0GQR1XS
NCI-SNU-1 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rSN2lEPTB;NkmwMlE4OiEQvF2= Mn\qV2FPT0WU
U-87-MG NIOzeJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnRToZoUUN3ME22PVQvPTh3IN88US=> MnzWV2FPT0WU
KM-H2 M3XNUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTlPZZKSzVyPU[5PU4xPTlizszN Mn2wV2FPT0WU
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BC-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknQTWM2OD16MEWuNlA{KM7:TR?= MnvUV2FPT0WU
NCI-H1155 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33idWlEPTB;OEG4MlA2QSEQvF2= M4XYUnNCVkeHUh?=
NCI-H1581 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3zfIJvUUN3ME25NFAvOjNzIN88US=> MmToV2FPT0WU

... 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:

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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 <1 mg/mL
In vivo 5% DMSO+30% PEG 300+ddH2O 24mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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. 252917-06-9 (free base)
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
    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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID