CHIR-99021 (CT99021) HCl

Catalog No.S2924

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 in cell-free assays; ability to distinguish between GSK-3 and 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 66 Publications

7 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.

  • 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 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM in cell-free assays; ability to distinguish between GSK-3 and 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 NGfGOoxHfW6ldHnvckBCe3OjeR?= MoXDN{DPxE1? NGXQ[Gw1KGh? MVnEUXNQ NH76NnZKdmirYnn0d{BxemWjZHnwc4N6fGViZHnm[oVz\W62aXH0bY9v MXKxNlA2PTJyMB?=
insulin receptor–expressing CHO-IR MYTGeY5kfGmxbjDBd5NigQ>? MWO1NFAhdk1? MV6zNEBucW5? MVPEUXNQ M3zQb2FkfGm4YYTld{BIdHmlb3flckBUgW62aHHz[UApT1Nr NHyxSWEyOjZyNkS5Oy=>
H4IIE M{TXW2Z2dmO2aX;uJGF{e2G7 NXPRdHFCOTBizszN NGDIPFczPCCq Mkf6SG1UVw>? NFfHNZZT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 NVnxfXB{OTV|NUCxPVU>
Oct4/Sox2/Klf4-infected MEFs MXfGeY5kfGmxbjDBd5NigQ>? Mn7zNVAh|ryP NX6yWIVxOjhiZB?= NG\3U4dFVVOR M2HpenBzd22xdHXzJG1GTnNicnXwdo9oemGvbXnu[{BVemGwc3T1Z4VlKGK7IF;jeFQtKFOxeEKsJIFv\CCNbH[0 MlTTNVk5OzlyNUW=
Sca-1+ HPC M{jhbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[yJO69VQ>? NWXQXHhRPiCm NEDGN5BFVVOR NUmzSVNHW3mwZYLnbZN1cWOjbHz5JJBzd22xdHXzJHNk[S1zK9MgTHBEKHC{b3zp[oVz[XSrb36gZY5lKGOxbH;ufUBnd3KvYYTpc44hfG:pZYTo[ZIhf2m2aDDFS2Y> NWK5NmJ5OjF4MkSzOFg>
HMC1.2 M{XUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fHWFMxKM7:TR?= MUG3NkBp NVPKboNHTE2VTx?= M2C4enJm\HWlZYOgZ4VtdCC|dYL2bZZidA>? NFu2OoszOjB|OUOwNS=>
Endothelial cell(EC) M1W0VWZ2dmO2aX;uJGF{e2G7 M1OxdVMh|ryP MX3EUXNQ M4r3OnBzd22xdHXzJIVv\G:2aHXsbYFtKGOnbHygLGVEMSCmaX\m[ZJmdnSrYYTpc44> MljZNlIxPTJyME[=
PANC1 M3fQcmFxd3C2b4Ppd{BCe3OjeR?= MkX3xsA2KM7:TR?= M1XXUFczKGh? M1PJU2ROW09? Mof0WJJq\2encoOgZY4h[XCxcITveIlkKHKnc4DvcpNm Mni4NlIzODFzOE[=
INS-1E NG\TT3ZHfW6ldHnvckBCe3OjeR?= MWOyMlUh|ryP M{i0flI1KGh? NFLl[3VFVVOR MWrJcoR2[2W|IHGgdoVlfWO2aX;uJI9nKE6SMTDveoVz\XiycnXzd4lwdg>? MnXGNlI1Ojd5MES=
hiPSC-NPs Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXoN-KBkc7:TR?= MWG3NkBp NHjGOIdFVVOR M1HDS2lv[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc47DqA>? MW[yNlY1OjZ6Nx?=
platelets M{m1XGZ2dmO2aX;uJGF{e2G7 MVmxNEDPxE1? NYjNW3BGOTVibXnu M1fIV2ROW09? NHi5WYVKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? NH;iPZczOzJ|OUi3Oy=>
DN3 NXfv[GNVTnWwY4Tpc44hSXO|YYm= MV2xNEDPxE1? MoDpPVYhcA>? M{OxZmROW09? NVO3SW46UW6lcnXhd4V{KGOnbHyg[IV3\WyxcH3lcpQh[W6mIIDyc4xq\mW{YYTpc44> MmnlNlM2OjZ7OEm=
embryonic stem cells (ESC) MVvGeY5kfGmxbjDBd5NigQ>? MVGzJOK2VQ>? MUexNUBl M{\LS2ROW09? M1m0XnBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= MnPJNlM5PDN|MUK=
H460 NEXaXHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK1JOK2VQ>? NW\C[mt6OjRiaB?= MmrhSG1UVw>? NELoZopRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> M4jkdVI1OzZ5Nki4
H157 M4K3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHyOUDDvU1? MUmyOEBp NXr1UpJsTE2VTx?= M3PXN3Bzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> M2PZTlI1OzZ5Nki4
H460 MnTWRZBweHSxc3nzJGF{e2G7 NXHUPHZ5PSEEtV2= MXyyOEBp NVLxWZJiTE2VTx?= NEPZXIVCfHSnboXheIV{KGOnbHygZZBweHSxc3nz M1Ls[VI1OzZ5Nki4
H157 M{D1R2Fxd3C2b4Ppd{BCe3OjeR?= NUK5WZlNPSEEtV2= NGHq[5UzPCCq M17XTmROW09? NF\adW1Fd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? M2S4OlI1OzZ5Nki4
A549 M2jXUmFxd3C2b4Ppd{BCe3OjeR?= NH;LWZI2KML3TR?= MVyyOEBp MXXEUXNQ Mn\4TY5kemWjc3XzJINmdGxiYYDvdJRwe2m| NEDKNnozPDN4N{[4PC=>
Neural progenitor cells M3\QS2Z2dmO2aX;uJGF{e2G7 Moq3N{DPxE1? MmTUNVAh\A>? NIHqPGlFVVOR MonMTY5lfWOnczDn[Y5memG2aX;uJI9nKG6ndYLhcEBxem:pZX7peI9zKGOnbHzz NFPkOpczPDZ|OECzOC=>
ES-D3 MoO0R5l1d3SxeHnjJGF{e2G7 MXixNOKh|ryP MkPWN{Bl MUPEUXNQ MULJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fUB4cXSqIFnDOVAhd2ZiND65JO69VQ>? MYqyOFc4QTN4NR?=
ES-CCE Ml\0R5l1d3SxeHnjJGF{e2G7 M1\K[lExyqEQvF2= M{LyfVMh\A>? M1L5NWROW09? NWOxbHRzUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHl? M4nJXlI1Pzd7M{[1
ES-D3 MojNSpVv[3Srb36gRZN{[Xl? MVS1xsDPxE1? M{jx[lMh\A>? MUjEUXNQ MV\TeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> NFy5WXEzPDd5OUO2OS=>
ES-CCE NVvYWoxDTnWwY4Tpc44hSXO|YYm= NYPVRZZtPcLizszN M1jTSVMh\A>? NH6yOW1FVVOR MYrTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> M2XNfFI1Pzd7M{[1
SW982 NW\tb5VQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV31SHFKUUN3ME2wMlIyPDF4IN88US=> MXvTRW5ITVJ?
GCT NF\SRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwM{C2O|Ih|ryP MkPlV2FPT0WU
769-P NHH0dIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX5TWM2OD1yLkW4OFk6KM7:TR?= NXfXfWo4W0GQR1XS
LOXIMVI MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7SWplDUUN3ME2wMlU5QDN{IN88US=> M1TCdHNCVkeHUh?=
D-336MG MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XPeWlEPTB;MD64OFYzKM7:TR?= M37leXNCVkeHUh?=
S-117 NWLyZYwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwOUKxN|Eh|ryP NUGzVHpbW0GQR1XS
D-247MG MmG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH6dItmUUN3ME2wMlk1QDV{IN88US=> Mlq1V2FPT0WU
TYK-nu MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPzN2RWUUN3ME2xMlA4QTF{IN88US=> NY\mdmdkW0GQR1XS
A498 Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrwepNKUUN3ME2xMlMxPDZ7IN88US=> MnSxV2FPT0WU
BCPAP Mn[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnI[HhlUUN3ME2xMlY3QDl6IN88US=> NEm5T|RUSU6JRWK=
KYSE-180 NF;YbFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwN{K3PFgh|ryP Mmn1V2FPT0WU
MIA-PaCa-2 NWHwU492T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHqWIlKSzVyPUGuO|U6PzdizszN NV;iXpdyW0GQR1XS
HCC1395 M2LIUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXxXIYzUUN3ME2xMlc5Ojd|IN88US=> NFTKVWRUSU6JRWK=
RS4-11 NWLC[mdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;mV2lEPTB;MT65OVQyPSEQvF2= NFn0NW5USU6JRWK=
NCI-H2122 NFy4foxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPadVM5UUN3ME2yMlI4Pjh2IN88US=> NUXlV3VrW0GQR1XS
SNU-423 NFfUXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJwNEm3PFch|ryP MWfTRW5ITVJ?
SK-LMS-1 NFzsNXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLNcYZKSzVyPUKuOlQyOjhizszN MVrTRW5ITVJ?
RPMI-7951 NHrCTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJwN{CxPVMh|ryP NET6S|dUSU6JRWK=
COLO-829 MlvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PhSmlEPTB;Mj63OlU1KM7:TR?= NWS0e3dkW0GQR1XS
SCC-9 NHnodXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M335NWlEPTB;Mj65OVQ5PSEQvF2= M3G5[nNCVkeHUh?=
A704 NVjCcZV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfwOpdKSzVyPUOuNFgyOiEQvF2= M{\qN3NCVkeHUh?=
HOP-62 NVvRZ|ZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2f4XWlEPTB;Mz6zOlA2PCEQvF2= NV3QcIw1W0GQR1XS
HCC1569 NYrT[Y5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\YTWM2OD1|LkS4N|A2KM7:TR?= M1e2OHNCVkeHUh?=
A172 NEPuOmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW1WYhqUUN3ME2zMlc2PDl6IN88US=> NU[4clV{W0GQR1XS
MOLT-16 NEiySXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm1[ZVHUUN3ME2zMlg5PTV4IN88US=> NGTWZppUSU6JRWK=
TE-15 M{LxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoO2TWM2OD1|Lkm1N|Q{KM7:TR?= M3jPXXNCVkeHUh?=
OE19 NEP0SYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULGPHBQUUN3ME2zMlk3PDVzIN88US=> M2XMenNCVkeHUh?=
MHH-ES-1 NHT0SnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PsWmlEPTB;ND6wOFU1PSEQvF2= MlnBV2FPT0WU
NKM-1 M4XRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTRwMUO5O|Eh|ryP NH\LVWhUSU6JRWK=
RCC10RGB NYLBXnJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHaUpJKSzVyPUSuNlk1PzlizszN NEj5eINUSU6JRWK=
BxPC-3 NXL1T49oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vGfWlEPTB;ND63NFM6OSEQvF2= MWLTRW5ITVJ?
ALL-PO NUXQTIFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u5O2lEPTB;ND64N|g2QCEQvF2= NV;QS2p[W0GQR1XS
SK-OV-3 NIf2e2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvlOZZQUUN3ME20Mlk6OzRizszN MmPaV2FPT0WU
SW1710 M3rIUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTVwNEK0OVYh|ryP NYPh[mZ7W0GQR1XS
NCI-H2452 NFvaWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PpOWlEPTB;NT60OVYzQCEQvF2= NF\TWXFUSU6JRWK=
D-392MG NF:xTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf4TWM2OD13LkS5NVQ2KM7:TR?= M4jIUHNCVkeHUh?=
LB2518-MEL NU\XVm1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3wTWdMUUN3ME21MlczPjJ5IN88US=> NHLRcYNUSU6JRWK=
BL-41 NETVVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XudmlEPTB;NT64NVI3PiEQvF2= NIXuZ41USU6JRWK=
WM-115 NGXKU|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\qSYxKSzVyPUWuPFE2ODlizszN MXzTRW5ITVJ?
SK-MEL-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7OTWM2OD14LkO4N|Q1KM7:TR?= NEfkTZpUSU6JRWK=
CGTH-W-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f0WmlEPTB;Nj60NVch|ryP M13kVHNCVkeHUh?=
BB65-RCC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiyb5RKSzVyPU[uOVMyQTVizszN M17rTHNCVkeHUh?=
CAL-85-1 NV;4dlB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PRbWlEPTB;Nj62NFk{PiEQvF2= Ml:4V2FPT0WU
RT-112 Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTdwMU[0OVYh|ryP M{nZVnNCVkeHUh?=
MC116 M3m5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rzOGlEPTB;Nz6yPFY6OSEQvF2= MlGzV2FPT0WU
G-361 NWW3blZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF6yVIxKSzVyPUeuOFY2PjFizszN MXvTRW5ITVJ?
SW1417 NV7rdFVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTJU2NPUUN3ME23MlY1PTh2IN88US=> NFfVXm1USU6JRWK=
MV-4-11 MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLZTWM2OD16LkW0N|A1KM7:TR?= NFvpRXNUSU6JRWK=
CAL-72 M1vaS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTnTWM2OD16Lke2NVE{KM7:TR?= M{DHcXNCVkeHUh?=
MKN28 NV7Memh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRThwOEi1NVYh|ryP M3HhdXNCVkeHUh?=
MEG-01 MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRThwOUmwOFMh|ryP MljvV2FPT0WU
ACHN NFnnOWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED5XJNKSzVyPUmuN|A2PDZizszN NYXxToY6W0GQR1XS
NCI-H1755 NWTOOIc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTlwM{m5PFYh|ryP M1TX[3NCVkeHUh?=
NCI-H64 NVjJT5JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HUPWlEPTB;OT60NlI2PSEQvF2= M{[0e3NCVkeHUh?=
COLO-205 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonzTWM2OD17LkSzPFIyKM7:TR?= MXTTRW5ITVJ?
CTV-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonnTWM2OD17LkSzPFk1KM7:TR?= M4PweXNCVkeHUh?=
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HuCCT1 NXTWUlVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WyUGlEPTB;NkeuNFM4PCEQvF2= MmPzV2FPT0WU
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EW-16 NF\1bo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHIR3RCUUN3ME23NU44PDF3IN88US=> MWnTRW5ITVJ?
KALS-1 MlO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvlfZZNUUN3ME23N{42PDd3IN88US=> MYHTRW5ITVJ?
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TE-12 NGXrbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW5fmR{UUN3ME24PU4{PzRzIN88US=> Ml;UV2FPT0WU
NCI-H650 M1K0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jaZ2lEPTB;OEmuPFczPCEQvF2= NF;IPFFUSU6JRWK=
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IGR-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTl7LkOxNVkh|ryP MXfTRW5ITVJ?
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PANC-08-13 NIPHcnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\uT2VKSzVyPUGwOk45PSEQvF2= NVTXTHM1W0GQR1XS
NCI-H23 NVHhWXN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFyOD6zOVch|ryP MW\TRW5ITVJ?
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D-263MG MmPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjVTWM2OD1zMEiuPVYyKM7:TR?= MYrTRW5ITVJ?
DU-145 NXzlUoZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTFyOT65OFUh|ryP NFXobYJUSU6JRWK=
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WSU-NHL MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTFzMj6wNUDPxE1? Mlv4V2FPT0WU
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MDA-MB-157 NFjNRZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3DeINnUUN3ME2xNVIvPDlizszN MnPRV2FPT0WU
NEC8 MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj1TWM2OD1zMUKuOlI1KM7:TR?= MmrxV2FPT0WU
SIG-M5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HTdWlEPTB;MUGzMlEzPSEQvF2= M3\VfnNCVkeHUh?=
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DMS-273 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFzNT62NVch|ryP NF\1W21USU6JRWK=
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HCC1599 Mn3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S5XmlEPTB;MUG3MlE2PiEQvF2= MXrTRW5ITVJ?
OVCAR-8 M4PNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjJ[mw4UUN3ME2xNVcvPjZ6IN88US=> M3zBeHNCVkeHUh?=
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KNS-81-FD Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;z[mlEPTB;MUG5MlQyPyEQvF2= NVW2VlhZW0GQR1XS
OVCAR-3 NGDlS5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\FO3V1UUN3ME2xNVkvQTF3IN88US=> MlWzV2FPT0WU
NCI-N87 NYT0Z|RlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfuTWM2OD1zMkGuNFQ1KM7:TR?= NVm3dnVUW0GQR1XS
HuP-T4 M17HNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36xeWlEPTB;MUKxMlU2KM7:TR?= NH\UdGNUSU6JRWK=
KYSE-140 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjufZZCUUN3ME2xNlIvOTRzIN88US=> NWrwO2tqW0GQR1XS
HAL-01 NV2xVph1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu0XHdZUUN3ME2xNlIvPDl7IN88US=> M1rWTHNCVkeHUh?=
HT-29 NXeyVZBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f5V2lEPTB;MUKyMlc4QCEQvF2= M37vdXNCVkeHUh?=
OPM-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLKSo9WUUN3ME2xNlMvOTd4IN88US=> MkjVV2FPT0WU
SW1463 NF:wR3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHGSFNKSzVyPUGyOE4xPzdizszN MYTTRW5ITVJ?
NCI-H2087 M4Tj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHEVpdFUUN3ME2xNlQvOjh|IN88US=> MniyV2FPT0WU
UMC-11 NHXXVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n3O2lEPTB;MUK2MlA{QCEQvF2= MWHTRW5ITVJ?
EB-3 M3jpb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXuclRRUUN3ME2xNlcvODF|IN88US=> MlHlV2FPT0WU
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NCI-H1581 M1i3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUGwNpRiUUN3ME25NFAvOjNzIN88US=> NVXXO|VRW0GQR1XS

... 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
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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

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

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Frequently Asked Questions

  • Question 1:

    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 2:

    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