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 74 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 NUHIPZJlTnWwY4Tpc44hSXO|YYm= M3\qelMh|ryP Mn3qOEBp NUTFe2E{TE2VTx?= MnTvTY5pcWKrdIOgdJJm[WSrcH;jfZRmKGSrZn\ldoVvfGmjdHnvci=> NFjUSXkyOjB3NUKwNC=>
insulin receptor–expressing CHO-IR NVPxV2J2TnWwY4Tpc44hSXO|YYm= M3m1WFUxOCCwTR?= NX[ydoZ6OzBibXnu NVG2RWZjTE2VTx?= M{XRXmFkfGm4YYTld{BIdHmlb3flckBUgW62aHHz[UApT1Nr MlT3NVI3ODZ2OUe=
H4IIE MWHGeY5kfGmxbjDBd5NigQ>? NHnFRmwyOCEQvF2= NWH1Z4dIOjRiaB?= Mk[1SG1UVw>? MoPRVoVofWyjdHXzJO6zNWOjdHXubY4h[WO2aY\peJkh[W6mIGTJVmUh[2:wdHHpcolv\yCycn;tc5RmeiCjY4Tpeol1gQ>? MnizNVU{PTBzOUW=
Oct4/Sox2/Klf4-infected MEFs NH3IOlRHfW6ldHnvckBCe3OjeR?= MVWxNEDPxE1? NUn2WY4zOjhiZB?= NV\oZoloTE2VTx?= MorLVJJwdW:2ZYOgUWVHeyC{ZYDyc4dz[W2vaX7nJHRz[W6|ZIXj[YQh[nliT3P0OEwhW2:6MjygZY5lKEuuZkS= M1P3OFE6QDN7MEW1
Sca-1+ HPC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzzSm0zKM7:TR?= MmTLOkBl NHj4VpZFVVOR M3PWXnN6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG NGHpcJMzOTZ{NEO0PC=>
HMC1.2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TkbVMxKM7:TR?= MkPhO|IhcA>? NYPHNoc4TE2VTx?= NHXRd5BT\WS3Y3XzJINmdGxic4Xyeol3[Wx? MYSyNlA{QTNyMR?=
Endothelial cell(EC) M1LBeGZ2dmO2aX;uJGF{e2G7 NEf6O5A{KM7:TR?= NUPOXFZNTE2VTx?= MX\Qdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u NVe0OZpIOjJyNUKwNFY>
PANC1 MWnBdI9xfG:|aYOgRZN{[Xl? M3i5eOKhPSEQvF2= NWjjSmxDPzJiaB?= NWGx[pNPTE2VTx?= NI\NfVNVemmpZ3Xyd{BidiCjcH;weI91cWNicnXzdI9ve2V? NXXycYJzOjJ{MEGxPFY>
INS-1E NWrhdJE6TnWwY4Tpc44hSXO|YYm= MX[yMlUh|ryP M2izVlI1KGh? M3u4XmROW09? M33PNmlv\HWlZYOgZUBz\WS3Y4Tpc44hd2ZiTmCxJI93\XKneIDy[ZN{cW:w MojWNlI1Ojd5MES=
hiPSC-NPs MlPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvBb5ZOO+LCid88US=> M1Xj[lczKGh? NGjKb3VFVVOR MkLHTY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh MVyyNlY1OjZ6Nx?=
platelets MmrnSpVv[3Srb36gRZN{[Xl? M4m0RlExKM7:TR?= MV2xOUBucW5? NGfMSmxFVVOR NH3XTpRKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? MXuyN|I{QTh5Nx?=
DN3 NFn2Wo1HfW6ldHnvckBCe3OjeR?= MlXWNVAh|ryP NInDc5I6PiCq M3\RVGROW09? M2Dtcmlv[3KnYYPld{Bk\WyuIHTleoVtd3CvZX70JIFv\CCycn;sbYZmemG2aX;u MkK4NlM2OjZ7OEm=
embryonic stem cells (ESC) MV;GeY5kfGmxbjDBd5NigQ>? NXT5WIJROyEEtV2= MUSxNUBl MlTsSG1UVw>? M1;JSHBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= MUCyN|g1OzNzMh?=
H460 Mon0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\nOUDDvU1? Ml3iNlQhcA>? NWfxO5h4TE2VTx?= MlvOVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u MVSyOFM3PzZ6OB?=
H157 NFLMZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYG1JOK2VQ>? MUKyOEBp NY\zc|h{TE2VTx?= NWjVeoxIWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v M2GwNVI1OzZ5Nki4
H460 M2\INWFxd3C2b4Ppd{BCe3OjeR?= MUG1JOK2VQ>? NVi2WmVyOjRiaB?= NEPBNY9FVVOR MUHBeJRmdnWjdHXzJINmdGxiYYDvdJRwe2m| M1jDelI1OzZ5Nki4
H157 M3KwWmFxd3C2b4Ppd{BCe3OjeR?= NI\IS4I2KML3TR?= MYqyOEBp NGPQUXZFVVOR MmLGSI9meyCwb4Sgd4lodmmoaXPhcpRtgSCjZn\lZ5Qh[XCxcITvd4l{ M3LNelI1OzZ5Nki4
A549 M4L2dmFxd3C2b4Ppd{BCe3OjeR?= M3vpelUhyrWP M4LaSFI1KGh? NHnFTZRFVVOR NVP5T4JWUW6lcnXhd4V{KGOnbHygZZBweHSxc3nz MVWyOFM3PzZ6OB?=
Neural progenitor cells MoX0SpVv[3Srb36gRZN{[Xl? NEXicmE{KM7:TR?= NUPGVFdSOTBiZB?= MlvjSG1UVw>? NHP6[ZdKdmS3Y3XzJIdmdmW{YYTpc44hd2ZibnX1doFtKHC{b3flcol1d3JiY3XscJM> MVeyOFY{QDB|NB?=
ES-D3 MU\DfZRwfG:6aXOgRZN{[Xl? NWPsV5plOTEEoN88US=> M{e2SFMh\A>? NVzLdmZZTE2VTx?= M3HLdGlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP NWP6UGZvOjR5N{mzOlU>
ES-CCE MXHDfZRwfG:6aXOgRZN{[Xl? NIHyXGoyOMLizszN MoLBN{Bl M{i5cmROW09? NHLOWnJKdmS3Y3XzJI1w\GW{YYTlJIN6fG:2b4jpZ4l1gQ>? NWX2O5k3OjR5N{mzOlU>
ES-D3 NVvnUmRNTnWwY4Tpc44hSXO|YYm= NFi3bpc2yqEQvF2= MUWzJIQ> MVfEUXNQ MXTTeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> MnfnNlQ4Pzl|NkW=
ES-CCE MXzGeY5kfGmxbjDBd5NigQ>? MYK1xsDPxE1? NIDXVIE{KGR? M1jjTWROW09? NFzNNVNUfHKxbnfsfUBqdmS3Y3XzJJRp\SCjY4Tpeol1gSCxZjDXcpQw[mW2YT3jZZRmdmmwIIDheIh4[Xl? Mn\nNlQ4Pzl|NkW=
SW982 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHtOIFKSzVyPUCuNlE1OTZizszN M2HtfnNCVkeHUh?=
GCT NI\CNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYG2NnJEUUN3ME2wMlMxPjd{IN88US=> M4LrW3NCVkeHUh?=
769-P NEPGb4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG1OJRQUUN3ME2wMlU5PDl7IN88US=> NV\2WXhFW0GQR1XS
LOXIMVI NFTYd4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojYTWM2OD1yLkW4PFMzKM7:TR?= NXLUV4hXW0GQR1XS
D-336MG MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwOES2NkDPxE1? NEjhcY9USU6JRWK=
S-117 NHrFPWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\RTVNKSzVyPUCuPVIyOzFizszN NXn3VY0zW0GQR1XS
D-247MG M4D0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPyTWM2OD1yLkm0PFUzKM7:TR?= Mo\1V2FPT0WU
TYK-nu MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDWfFRXUUN3ME2xMlA4QTF{IN88US=> M4nqTXNCVkeHUh?=
A498 NUT2NZVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwM{C0Olkh|ryP MV;TRW5ITVJ?
BCPAP NHX5UJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDEWXR3UUN3ME2xMlY3QDl6IN88US=> M4H5bHNCVkeHUh?=
KYSE-180 M1vq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO0TWM2OD1zLkeyO|g5KM7:TR?= NFfvd4lUSU6JRWK=
MIA-PaCa-2 MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHLTWM2OD1zLke1PVc4KM7:TR?= MlHMV2FPT0WU
HCC1395 M4rheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn5UGVwUUN3ME2xMlc5Ojd|IN88US=> NXqwRXQ2W0GQR1XS
RS4-11 M1vXbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSwdFFuUUN3ME2xMlk2PDF3IN88US=> Mnu3V2FPT0WU
NCI-H2122 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjpe3MzUUN3ME2yMlI4Pjh2IN88US=> M2fuVHNCVkeHUh?=
SNU-423 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPjW4tKSzVyPUKuOFk4QDdizszN MXzTRW5ITVJ?
SK-LMS-1 M4LoWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jjT2lEPTB;Mj62OFEzQCEQvF2= NX7UbW1GW0GQR1XS
RPMI-7951 NW\QeHdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrSU2VKSzVyPUKuO|AyQTNizszN M{C1[XNCVkeHUh?=
COLO-829 NUXXR3o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfYcoJKSzVyPUKuO|Y2PCEQvF2= MXjTRW5ITVJ?
SCC-9 MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvCOlVKSzVyPUKuPVU1QDVizszN MnjrV2FPT0WU
A704 MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\ZNWU4UUN3ME2zMlA5OTJizszN NHvpb2NUSU6JRWK=
HOP-62 NGPUblhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXTRWJKSzVyPUOuN|YxPTRizszN NVL1eZFwW0GQR1XS
HCC1569 NVHvXI5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXS4fHBRUUN3ME2zMlQ5OzB3IN88US=> MWnTRW5ITVJ?
A172 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrETWM2OD1|Lke1OFk5KM7:TR?= NHK1RmNUSU6JRWK=
MOLT-16 NXzRem5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLpTmVjUUN3ME2zMlg5PTV4IN88US=> M3TaUHNCVkeHUh?=
TE-15 NYnyNmRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TDbWlEPTB;Mz65OVM1OyEQvF2= MXTTRW5ITVJ?
OE19 M{TwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVmyXoRuUUN3ME2zMlk3PDVzIN88US=> M3vYO3NCVkeHUh?=
MHH-ES-1 NXfF[GVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTRwMES1OFUh|ryP MVzTRW5ITVJ?
NKM-1 M1PScmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrVeVJzUUN3ME20MlE{QTdzIN88US=> MWDTRW5ITVJ?
RCC10RGB NUHpbnZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHNVI1KSzVyPUSuNlk1PzlizszN MlzsV2FPT0WU
BxPC-3 M3\lTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHpNpFKSzVyPUSuO|A{QTFizszN NFXsSY5USU6JRWK=
ALL-PO NFviTlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O1d2lEPTB;ND64N|g2QCEQvF2= NH7mVmlUSU6JRWK=
SK-OV-3 M3TVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTwWVVYUUN3ME20Mlk6OzRizszN NVzkfZE6W0GQR1XS
SW1710 NHLmPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTVwNEK0OVYh|ryP NILZW|BUSU6JRWK=
NCI-H2452 NG\ndlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XnXWlEPTB;NT60OVYzQCEQvF2= MniyV2FPT0WU
D-392MG MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n6RmlEPTB;NT60PVE1PSEQvF2= NV[5[pZMW0GQR1XS
LB2518-MEL MmnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD6cXlXUUN3ME21MlczPjJ5IN88US=> NEGx[IpUSU6JRWK=
BL-41 MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTVwOEGyOlYh|ryP M1nEUHNCVkeHUh?=
WM-115 NWPJWFBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfGTWM2OD13LkixOVA6KM7:TR?= NWnBRlhvW0GQR1XS
SK-MEL-2 M2LrbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn4XWhKSzVyPU[uN|g{PDRizszN MkfYV2FPT0WU
CGTH-W-1 NF;IbXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvnWmZKSzVyPU[uOFE4KM7:TR?= MU\TRW5ITVJ?
BB65-RCC MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q4bWlEPTB;Nj61N|E6PSEQvF2= NFrLZ|FUSU6JRWK=
CAL-85-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j1cGlEPTB;Nj62NFk{PiEQvF2= MorIV2FPT0WU
RT-112 M4HjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPVbXpKSzVyPUeuNVY1PTZizszN NHvxN|JUSU6JRWK=
MC116 NUPSWGlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK4TWM2OD15LkK4OlkyKM7:TR?= NIWxe|NUSU6JRWK=
G-361 M1LtOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTdwNE[1OlEh|ryP MVrTRW5ITVJ?
SW1417 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWS4fpdlUUN3ME23MlY1PTh2IN88US=> NUTURotFW0GQR1XS
MV-4-11 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRThwNUSzNFQh|ryP MYXTRW5ITVJ?
CAL-72 Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluyTWM2OD16Lke2NVE{KM7:TR?= MmLFV2FPT0WU
MKN28 NWDQdVliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRThwOEi1NVYh|ryP MoLZV2FPT0WU
MEG-01 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTyTphKSzVyPUiuPVkxPDNizszN M1PwTHNCVkeHUh?=
ACHN MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vJUmlEPTB;OT6zNFU1PiEQvF2= MlLiV2FPT0WU
NCI-H1755 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHG0T|lKSzVyPUmuN|k6QDZizszN MVrTRW5ITVJ?
NCI-H64 MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTlwNEKyOVUh|ryP M13CSnNCVkeHUh?=
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U-2-OS NVjP[2hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHydY1KUUN3ME25MlQ2ODB4IN88US=> Mn3VV2FPT0WU
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SF539 M3XlNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrVZWtOUUN3ME2xOE4xOTF4IN88US=> Mon1V2FPT0WU
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Daudi NI\4SWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTGb3ZLUUN3ME2xO{43OTR7IN88US=> MXvTRW5ITVJ?
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NCI-H1770 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L5fmlEPTB;Mk[uPFk5PiEQvF2= M2r2dnNCVkeHUh?=
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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