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 71 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.

    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.

  • 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 M1K5VGZ2dmO2aX;uJGF{e2G7 MkSwN{DPxE1? NGL0R|g1KGh? MYrEUXNQ M2SwXWlvcGmkaYTzJJBz\WGmaYDvZ5l1\SCmaX\m[ZJmdnSrYYTpc44> NXTN[VRUOTJyNUWyNFA>
insulin receptor–expressing CHO-IR Mn;lSpVv[3Srb36gRZN{[Xl? NVTj[XN7PTByIH7N M1joO|MxKG2rbh?= M4r4W2ROW09? NWfo[mJ4SWO2aY\heIV{KEeueXPv[4VvKFO7boToZZNmKCiJUzm= M17R[FEzPjB4NEm3
H4IIE NVTIWZdsTnWwY4Tpc44hSXO|YYm= M1\WZVExKM7:TR?= M376XFI1KGh? NWfsV|Z[TE2VTx?= NXTnTHkyWmWpdXzheIV{KM7{LXPheIVvcW5iYXP0bZZqfHliYX7kJHRKWkViY3;ueIFqdmmwZzDwdo9ud3SncjDhZ5Rqfmm2eR?= MlHONVU{PTBzOUW=
Oct4/Sox2/Klf4-infected MEFs NH\wXIhHfW6ldHnvckBCe3OjeR?= NGL6[lQyOCEQvF2= NVHUT4J4OjhiZB?= M4X6[WROW09? M1XYOXBzd22xdHXzJG1GTnNicnXwdo9oemGvbXnu[{BVemGwc3T1Z4VlKGK7IF;jeFQtKFOxeEKsJIFv\CCNbH[0 MlvVNVk5OzlyNUW=
Sca-1+ HPC MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTtNkDPxE1? NFfZfZA3KGR? NH\I[XpFVVOR M1[0U3N6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG MYOyNVYzPDN2OB?=
HMC1.2 NXfvXpBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\FR5k{OCEQvF2= MXK3NkBp NIq2WIpFVVOR NV3YZYVTWmWmdXPld{Bk\WyuIIP1dpZqfmGu MWSyNlA{QTNyMR?=
Endothelial cell(EC) MX3GeY5kfGmxbjDBd5NigQ>? MWGzJO69VQ>? MnzuSG1UVw>? MnrNVJJwdW:2ZYOg[Y5ld3SqZXzpZYwh[2WubDCoSWMqKGSrZn\ldoVvfGmjdHnvci=> M4\Vb|IzODV{MEC2
PANC1 NEP2WJJCeG:ydH;zbZMhSXO|YYm= MV9CpFUh|ryP MnjkO|IhcA>? NVf1dmpRTE2VTx?= MWDUdolo\2W{czDhckBieG:ydH;0bYMhemW|cH;ud4U> NUnDfI5iOjJ{MEGxPFY>
INS-1E M37lemZ2dmO2aX;uJGF{e2G7 MlLYNk42KM7:TR?= MmrsNlQhcA>? NGPxNoZFVVOR NXLZdGZOUW6mdXPld{BiKHKnZIXjeIlwdiCxZjDOVFEhd3[ncnX4dJJme3Orb36= NFHIR4ozOjR{N{ewOC=>
hiPSC-NPs NIOxOnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzzTW0{6oDLzszN MorpO|IhcA>? NXLDZWJUTE2VTx?= NYnQ[GlqUW6lcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdsLi MWGyNlY1OjZ6Nx?=
platelets NF;hXoRHfW6ldHnvckBCe3OjeR?= MUCxNEDPxE1? M3\vclE2KG2rbh?= NXHa[pZRTE2VTx?= NFjKUYNKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? MWGyN|I{QTh5Nx?=
DN3 NInOTpNHfW6ldHnvckBCe3OjeR?= MojRNVAh|ryP NXPIfWFCQTZiaB?= MljuSG1UVw>? NXnCeoJYUW6lcnXhd4V{KGOnbHyg[IV3\WyxcH3lcpQh[W6mIIDyc4xq\mW{YYTpc44> NH7F[3gzOzV{Nkm4PS=>
embryonic stem cells (ESC) NV\1To5VTnWwY4Tpc44hSXO|YYm= MorCN{DDvU1? NFvZZ5MyOSCm NEfBXYZFVVOR MUPQdo9ud3SnczDz[YxnNXKnbnX3ZYwhd2ZibnJDs5ZmNXS7cHWgcY92e2ViZX3idplwdmmlIIP0[Y0h[2WubIOgLGVUSyl? NVqweVhiOjN6NEOzNVI>
H460 MoPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3f4WFUhyrWP MV6yOEBp NYf3To9nTE2VTx?= NGrXWXlRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> MWiyOFM3PzZ6OB?=
H157 NYPvSVY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH0OUDDvU1? M3LyclI1KGh? NF3sSW1FVVOR MkPhVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u MYeyOFM3PzZ6OB?=
H460 NXvMToM1SXCxcITvd4l{KEG|c3H5 M{T1WlUhyrWP NXPnZXREOjRiaB?= MWHEUXNQ NHLLZYtCfHSnboXheIV{KGOnbHygZZBweHSxc3nz M4TYd|I1OzZ5Nki4
H157 NVr0SZA2SXCxcITvd4l{KEG|c3H5 MorqOUDDvU1? MnjzNlQhcA>? MXLEUXNQ NU\Uc4RCTG:nczDuc5Qhe2mpbnnmbYNidnSueTDh[oZm[3RiYYDvdJRwe2m| M2fzS|I1OzZ5Nki4
A549 NIHkNo5CeG:ydH;zbZMhSXO|YYm= M2G2OlUhyrWP NIPiTIMzPCCq NHLTU2tFVVOR NYr3[2drUW6lcnXhd4V{KGOnbHygZZBweHSxc3nz M2L5NVI1OzZ5Nki4
Neural progenitor cells NHTy[W5HfW6ldHnvckBCe3OjeR?= MonMN{DPxE1? MXSxNEBl M4TyZWROW09? M{C3SWlv\HWlZYOg[4Vv\XKjdHnvckBw\iCwZYXyZYwheHKxZ3XubZRweiClZXzsdy=> Mn[1NlQ3OzhyM{S=
ES-D3 MVHDfZRwfG:6aXOgRZN{[Xl? M2TofFExyqEQvF2= NUnpXIg2OyCm NGDObHdFVVOR M{mzZmlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP NEDaOHkzPDd5OUO2OS=>
ES-CCE MVHDfZRwfG:6aXOgRZN{[Xl? MXmxNOKh|ryP MUKzJIQ> MVrEUXNQ MmrhTY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJk> MUWyOFc4QTN4NR?=
ES-D3 M2nUemZ2dmO2aX;uJGF{e2G7 M4jm[VXDqM7:TR?= NXXuSZN2OyCm MnfGSG1UVw>? NUjoVpp5W3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 MW[yOFc4QTN4NR?=
ES-CCE NI\nU4xHfW6ldHnvckBCe3OjeR?= NEXCN4c2yqEQvF2= M2O1clMh\A>? MWrEUXNQ NUPw[VhqW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 Mo\XNlQ4Pzl|NkW=
SW982 NIjsN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjDdVdKSzVyPUCuNlE1OTZizszN MXvTRW5ITVJ?
GCT MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\xVpRKSzVyPUCuN|A3PzJizszN M2nUNHNCVkeHUh?=
769-P M4jzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwNUi0PVkh|ryP NF62TWJUSU6JRWK=
LOXIMVI MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTpfZBKSzVyPUCuOVg5OzJizszN NFm0WHZUSU6JRWK=
D-336MG NWjNO|BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInIeGtKSzVyPUCuPFQ3OiEQvF2= NGHrbHBUSU6JRWK=
S-117 NHfw[|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXZR5NkUUN3ME2wMlkzOTNzIN88US=> MVnTRW5ITVJ?
D-247MG Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDqTWM2OD1yLkm0PFUzKM7:TR?= MXjTRW5ITVJ?
TYK-nu NGTjRWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;sTWM2OD1zLkC3PVEzKM7:TR?= M3;EWHNCVkeHUh?=
A498 Mnu3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwM{C0Olkh|ryP NX\0TJBrW0GQR1XS
BCPAP NE\1TIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG1TWM2OD1zLk[2PFk5KM7:TR?= MYfTRW5ITVJ?
KYSE-180 M{DL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHzTWM2OD1zLkeyO|g5KM7:TR?= MoXCV2FPT0WU
MIA-PaCa-2 Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\HTWM2OD1zLke1PVc4KM7:TR?= NV3ES5JWW0GQR1XS
HCC1395 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\TVml2UUN3ME2xMlc5Ojd|IN88US=> NXjEW5pYW0GQR1XS
RS4-11 NHnGPW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwOUW0NVUh|ryP NYTOclRGW0GQR1XS
NCI-H2122 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojHTWM2OD1{LkK3Olg1KM7:TR?= M1vVT3NCVkeHUh?=
SNU-423 NXzFWmVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwNEm3PFch|ryP M3vnfnNCVkeHUh?=
SK-LMS-1 NUPLXZBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzGTWM2OD1{Lk[0NVI5KM7:TR?= NELmcWlUSU6JRWK=
RPMI-7951 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjZVYxSUUN3ME2yMlcxOTl|IN88US=> MWHTRW5ITVJ?
COLO-829 NXH4RnFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjnTWM2OD1{Lke2OVQh|ryP NYrmZnZuW0GQR1XS
SCC-9 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTBTWM2OD1{Lkm1OFg2KM7:TR?= MVHTRW5ITVJ?
A704 NIrjOIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\TUIkzUUN3ME2zMlA5OTJizszN MnjBV2FPT0WU
HOP-62 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrESGxZUUN3ME2zMlM3ODV2IN88US=> NXvnTGN[W0GQR1XS
HCC1569 NIHYZYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF6yTHVKSzVyPUOuOFg{ODVizszN MknNV2FPT0WU
A172 NFHiXlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O0dGlEPTB;Mz63OVQ6QCEQvF2= MUDTRW5ITVJ?
MOLT-16 Mmr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTNwOEi1OVYh|ryP NIHi[llUSU6JRWK=
TE-15 NHrmVnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fBemlEPTB;Mz65OVM1OyEQvF2= MX7TRW5ITVJ?
OE19 M{[5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrJWpNxUUN3ME2zMlk3PDVzIN88US=> MX3TRW5ITVJ?
MHH-ES-1 M3TZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTlTZRKSzVyPUSuNFQ2PDVizszN NUTiWnZEW0GQR1XS
NKM-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfCTlJzUUN3ME20MlE{QTdzIN88US=> MkHVV2FPT0WU
RCC10RGB MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWOzXGNGUUN3ME20MlI6PDd7IN88US=> M3jtXnNCVkeHUh?=
BxPC-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfDOYpKSzVyPUSuO|A{QTFizszN NUWzPVJPW0GQR1XS
ALL-PO NYfqS5BoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILn[mpKSzVyPUSuPFM5PThizszN M2PoNHNCVkeHUh?=
SK-OV-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTRwOUmzOEDPxE1? MmTlV2FPT0WU
SW1710 NF36ZnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe5O4lKSzVyPUWuOFI1PTZizszN MlTiV2FPT0WU
NCI-H2452 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTVwNEW2Nlgh|ryP NX7tS4poW0GQR1XS
D-392MG M3fDRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTVwNEmxOFUh|ryP M{XLXnNCVkeHUh?=
LB2518-MEL Mmq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\5TWM2OD13LkeyOlI4KM7:TR?= NVOwZlVyW0GQR1XS
BL-41 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLhTWM2OD13LkixNlY3KM7:TR?= NVjobJhEW0GQR1XS
WM-115 M2HLWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\jNHR7UUN3ME21MlgyPTB7IN88US=> M1q1ZXNCVkeHUh?=
SK-MEL-2 NXqweo1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTuTWM2OD14LkO4N|Q1KM7:TR?= NEeybHVUSU6JRWK=
CGTH-W-1 NX3NSI9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vYdWlEPTB;Nj60NVch|ryP NWjjdVNpW0GQR1XS
BB65-RCC NIHsT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zyb2lEPTB;Nj61N|E6PSEQvF2= M3fGR3NCVkeHUh?=
CAL-85-1 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HaZmlEPTB;Nj62NFk{PiEQvF2= NET6TIFUSU6JRWK=
RT-112 M17pd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP2TWM2OD15LkG2OFU3KM7:TR?= NUm3TohwW0GQR1XS
MC116 M3L2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DOUGlEPTB;Nz6yPFY6OSEQvF2= MXXTRW5ITVJ?
G-361 NFf5RYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDJPHFyUUN3ME23MlQ3PTZzIN88US=> NIjJTopUSU6JRWK=
SW1417 NV\NcXI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTdwNkS1PFQh|ryP NVvmSXFqW0GQR1XS
MV-4-11 NFHIVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknXTWM2OD16LkW0N|A1KM7:TR?= NY\H[5dOW0GQR1XS
CAL-72 NGDzOZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HnZWlEPTB;OD63OlEyOyEQvF2= Mm\YV2FPT0WU
MKN28 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\5dmlEPTB;OD64PFUyPiEQvF2= M3X0W3NCVkeHUh?=
MEG-01 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XkdGlEPTB;OD65PVA1OyEQvF2= NF2xPGVUSU6JRWK=
ACHN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTlwM{C1OFYh|ryP MnfJV2FPT0WU
NCI-H1755 M3HTVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTmTWM2OD17LkO5PVg3KM7:TR?= NGXTeHpUSU6JRWK=
NCI-H64 MoLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTlwNEKyOVUh|ryP MoX2V2FPT0WU
COLO-205 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzPN44xUUN3ME25MlQ{QDJzIN88US=> M{fQdXNCVkeHUh?=
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NCI-H2171 NE\Y[5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vjd2lEPTB;NUGyMlcxPSEQvF2= MWjTRW5ITVJ?
Mo-T MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTVzNT6xNVYh|ryP Mm[0V2FPT0WU
HL-60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7EZ5RJUUN3ME21NlIvQTJ2IN88US=> NUO1e3RJW0GQR1XS
NCI-H1436 NIWybJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTV{Mz6wOlQh|ryP MWLTRW5ITVJ?
NCI-H510A NHHyRXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjWXGZFUUN3ME21NlQvPjl4IN88US=> MWfTRW5ITVJ?
NCI-H2081 NE[weJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX3TWM2OD13MkWuOVE{KM7:TR?= M{DkZ3NCVkeHUh?=
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NCI-H2227 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfSTWM2OD13M{CuNlU1KM7:TR?= MkDSV2FPT0WU
HSC-4 NX7LfXVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDSUW5KSzVyPUWzPU4zQTNizszN M3LRZ3NCVkeHUh?=
RL NHK0PWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk[1TWM2OD13NEKuOFQzKM7:TR?= NYDKNlRkW0GQR1XS
EVSA-T M1PFeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHq[|ZRUUN3ME21OFMvPjh2IN88US=> NEC2UXhUSU6JRWK=
NCI-H889 M3fse2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3MfFBGUUN3ME21OFcvOjNizszN NHrzNJFUSU6JRWK=
COLO-320-HSR MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T5emlEPTB;NUWxMlM2KM7:TR?= MX\TRW5ITVJ?
EW-11 NHPpSWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTV3Mj6zPVkh|ryP NVzrZ3pyW0GQR1XS
UACC-812 Mn\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTG[|BPUUN3ME21OVkvOzlzIN88US=> MnHGV2FPT0WU
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HT NXro[XBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTRS5JvUUN3ME22NlIvPzh3IN88US=> M1LkRnNCVkeHUh?=
NCI-H226 Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml60TWM2OD14MkiuN|U{KM7:TR?= MmTJV2FPT0WU
L-363 NUi0coxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTZ2OD6wOlQh|ryP NHHVNpVUSU6JRWK=
IM-9 MmDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOyd4N6UUN3ME22OVEvPTRzIN88US=> M4TaVXNCVkeHUh?=
TUR M4frN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGz[|RKSzVyPU[3NU4{OjJizszN M2HVdXNCVkeHUh?=
NCI-SNU-16 M2fsd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPhZmFKSzVyPU[4NE41PjJizszN NYH5S5h7W0GQR1XS
NCI-SNU-1 MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTZ7MD6xO|Ih|ryP MnXQV2FPT0WU
U-87-MG NFK0fYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXPUnpKSzVyPU[5OE42QDVizszN MYrTRW5ITVJ?
KM-H2 MmnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v4b2lEPTB;Nkm5MlA2QSEQvF2= Ml3RV2FPT0WU
DEL MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWr1U5lnUUN3ME23NFAvQDN6IN88US=> M4rPS3NCVkeHUh?=
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BC-3 NH22RnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXzTWM2OD16MEWuNlA{KM7:TR?= NGfBOmhUSU6JRWK=
NCI-H1155 NUnnfZFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRThzOD6wOVkh|ryP NVfqNHdWW0GQR1XS
NCI-H1581 M1TR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;kTotKSzVyPUmwNE4zOzFizszN MlLvV2FPT0WU

... 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 Insoluble
In vivo Add solvents to the product individually and in order:
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
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:

    I recently purchased CHIR 99021 to inject mice intraperitoneally. The data sheet says using 10% captisol for in vivo use. Is it for IP injection? Or do you have other solutions to suggest to use for in vivo IP injection of CHIR 99021?

  • Answer:

    The formulation of 15% Captisol is for oral gavage, and S2924 CHIR-99021 (CT99021) HCl in it is a suspension. S2924 CHIR-99021 (CT99021) HCl can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 24mg/ml as a clear solution for IP injection.

  • Question 2:

    How about the half-life of this compound? If it is necessary for daily treatment when the compound is used in long-term experiment?

  • Answer:

    Please change the culture medium each day to add the new comound in it if the duration is more than 72h.

  • Question 3:

    What is the difference between S2924 and S1263? Which one is better for differentiation?

  • Answer:

    S1263 is the free base format of Chir-99021, while S2924 is the HCl salt format. They have the same biological activity but are slightly different in solubility.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID