CHIR-99021 (CT99021) HCl

目录号:S2924

CHIR-99021 (CT99021) HCl Chemical Structure

Molecular Weight(MW): 501.8

CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂,IC50为10 nM/6.7 nM。 其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。

规格 价格 库存 购买数量  
RMB 2780.99 现货
RMB 733.53 现货
RMB 1373.92 现货
RMB 4650.09 现货
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客户购买Selleck的此次产品后发表的文献70篇:

客户使用该产品的9个实验数据:

  • 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.

产品安全说明书

GSK-3抑制剂选择性比较

生物活性

产品描述 CHIR-99021 (CT99021) HCl是CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂,IC50为10 nM/6.7 nM。 其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。
靶点
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
体外研究

CHIR-99021作用于GSK-3比作用于其最接近的同系物CDC2和ERK2,及其他蛋白激酶选择性高500倍。此外,CHIR-99021只与一组22种药理相关的受体微弱结合,且对一组23种非激酶的酶几乎没有抑制活性。CHIR-99021作用于表达胰岛素受体的CHO-IR细胞,诱导糖原合成酶(GS)激活,EC50为0.763 μM。[1]CHIR-99021(3 μM)作用于3T3-L1前脂肪细胞,除了模拟胰岛素的作用,抑制GSK-3,使胞内游离β-catenin增加1.9倍,模仿经典Wnt信号通路。在分化的前3天,CHIR-99021处理,抑制脂肪细胞分化,IC50为0.3 μM,通过抑制CCAAT/增强子结合蛋白α(C/EBPα)和过氧化物酶体增殖物激活受体γ(PPARγ)的诱导作用。[2] 不像LiCl和AR-A014418,CHIR-99021处理,即使在高浓度,不会降低INS-1E细胞活力。相反,CHIR-99021增加INS-1E细胞增殖,这种作用具有剂量依赖性,且显著抑制高糖和高棕榈酸诱导的INS-E细胞死亡,这种作用具有浓度依赖性。CHIR-99021浓度低至1 μM,处理离体大鼠胰岛,促进β细胞复制,5 μM CHIR-99021处理,使细胞复制增长2-3倍。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3-L1 MX\GeY5kfGmxbjDBd5NigQ>? Mkj4N{DPxE1? MWi0JIg> NHLzfWVFVVOR NH7MOlVKdmirYnn0d{BxemWjZHnwc4N6fGViZHnm[oVz\W62aXH0bY9v MVmxNlA2PTJyMB?=
insulin receptor–expressing CHO-IR NEPTd2NHfW6ldHnvckBCe3OjeR?= M3LUSFUxOCCwTR?= M1T2NFMxKG2rbh?= NUi4cXc5TE2VTx?= MnG1RYN1cX[jdHXzJGdtgWOxZ3XuJHN6dnSqYYPlJEhIWyl? MlPyNVI3ODZ2OUe=
H4IIE NEPIeJdHfW6ldHnvckBCe3OjeR?= Mne4NVAh|ryP NXL4cpp5OjRiaB?= NYnrUJpSTE2VTx?= MWPS[Yd2dGG2ZYOg{tIu[2G2ZX7pckBi[3Srdnn0fUBidmRiVFnSSUBkd262YXnubY5oKHC{b33veIVzKGGldHn2bZR6 NXrUR4RTOTV|NUCxPVU>
Oct4/Sox2/Klf4-infected MEFs NFK4RVFHfW6ldHnvckBCe3OjeR?= NInDUlUyOCEQvF2= M1Xw[|I5KGR? NGfFOJVFVVOR M3HLc3Bzd22xdHXzJG1GTnNicnXwdo9oemGvbXnu[{BVemGwc3T1Z4VlKGK7IF;jeFQtKFOxeEKsJIFv\CCNbH[0 NV3lc3B{OTl6M{mwOVU>
Sca-1+ HPC NE\iOZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HncVIh|ryP NE[0SVg3KGR? MX\EUXNQ MoTMV5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NYS0VWxpOjF4MkSzOFg>
HMC1.2 M2XOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HMb|MxKM7:TR?= NWPhbnhDPzJiaB?= NUPOUHkxTE2VTx?= MnHhVoVlfWOnczDj[YxtKHO3co\peoFt M1XYc|IzODN7M{Cx
Endothelial cell(EC) NYPEVYE1TnWwY4Tpc44hSXO|YYm= NW\IcZZEOyEQvF2= MnnCSG1UVw>? NI[yb4RRem:vb4Tld{BmdmSxdHjlcIlidCClZXzsJEhGSyliZHnm[oVz\W62aXH0bY9v MkLlNlIxPTJyME[=
PANC1 MkjrRZBweHSxc3nzJGF{e2G7 M3v4VeKhPSEQvF2= NVriRlloPzJiaB?= NFfDNW5FVVOR MV;Udolo\2W{czDhckBieG:ydH;0bYMhemW|cH;ud4U> M3nnU|IzOjBzMUi2
INS-1E NUfDSIRPTnWwY4Tpc44hSXO|YYm= M37ycFIvPSEQvF2= NX7HZYRtOjRiaB?= M1fyd2ROW09? NEi5UIdKdmS3Y3XzJIEhemWmdXP0bY9vKG:oIF7QNUBwfmW{ZYjwdoV{e2mxbh?= NHnNOZUzOjR{N{ewOC=>
hiPSC-NPs Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUT3bZJEO+LCid88US=> MYO3NkBp M4SzN2ROW09? MlPCTY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh MVGyNlY1OjZ6Nx?=
platelets MWrGeY5kfGmxbjDBd5NigQ>? MUGxNEDPxE1? M2TRR|E2KG2rbh?= NFrweYpFVVOR NE\Fd2lKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? NGr2RYYzOzJ|OUi3Oy=>
DN3 NHnUbXFHfW6ldHnvckBCe3OjeR?= MXuxNEDPxE1? NGrIeoI6PiCq M1fa[2ROW09? MYDJcoNz\WG|ZYOgZ4VtdCCmZY\lcI9xdWWwdDDhcoQheHKxbHnm[ZJifGmxbh?= NXTCZ5k6OjN3Mk[5PFk>
embryonic stem cells (ESC) MmTSSpVv[3Srb36gRZN{[Xl? NXjwXWw6OyEEtV2= M4P4UlEyKGR? NUjUVmlJTE2VTx?= NFfoc2pRem:vb4Tld{B{\WyoLYLlcoV4[Wxib3[gcoHEt3[nLYT5dIUhdW:3c3Wg[Y1jenmxbnnjJJN1\W1iY3XscJMhMEWVQzm= NX;FNIVrOjN6NEOzNVI>
H460 NUHCTW9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi1JOK2VQ>? NFL0NGUzPCCq NUTSenFUTE2VTx?= NWCzZ|JVWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v NHXyeZUzPDN4N{[4PC=>
H157 M4HZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrPOUDDvU1? M2rSb|I1KGh? NETMZmdFVVOR MW\Qdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= MoXtNlQ{Pjd4OEi=
H460 M33qPGFxd3C2b4Ppd{BCe3OjeR?= Mn64OUDDvU1? NXLn[YNjOjRiaB?= NGn4OmNFVVOR NFTPN45CfHSnboXheIV{KGOnbHygZZBweHSxc3nz M2nZWFI1OzZ5Nki4
H157 NIfzNllCeG:ydH;zbZMhSXO|YYm= NIP1c|Q2KML3TR?= MnzXNlQhcA>? NXT3OmNXTE2VTx?= NH\0W2tFd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? MnO5NlQ{Pjd4OEi=
A549 NF;iWFRCeG:ydH;zbZMhSXO|YYm= MofvOUDDvU1? MkS4NlQhcA>? M2PacmROW09? NHrzRXFKdmO{ZXHz[ZMh[2WubDDhdI9xfG:|aYO= NYG2Xoh[OjR|Nke2PFg>
Neural progenitor cells Mlr2SpVv[3Srb36gRZN{[Xl? NFO5XGE{KM7:TR?= M3LvOVExKGR? M3PCNmROW09? MYnJcoR2[2W|IHflcoVz[XSrb36gc4YhdmW3cnHsJJBzd2enbnn0c5Ih[2WubIO= MmnRNlQ3OzhyM{S=
ES-D3 M1nyUWN6fG:2b4jpZ{BCe3OjeR?= MknmNVDDqM7:TR?= NV\u[o44OyCm M1j1XWROW09? M13PcWlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP MWCyOFc4QTN4NR?=
ES-CCE NIP5dmVEgXSxdH;4bYMhSXO|YYm= NF3K[|UyOMLizszN M4fLflMh\A>? MYLEUXNQ MkXGTY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJk> Mk\qNlQ4Pzl|NkW=
ES-D3 MkXNSpVv[3Srb36gRZN{[Xl? NELKPYo2yqEQvF2= MWKzJIQ> NYm3ZVRPTE2VTx?= NYm1SFlqW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 M4DubFI1Pzd7M{[1
ES-CCE MYDGeY5kfGmxbjDBd5NigQ>? NVzaOGlZPcLizszN M1\CR|Mh\A>? MnzUSG1UVw>? MlWxV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 MXKyOFc4QTN4NR?=
SW982 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\OTWM2OD1yLkKxOFE3KM7:TR?= NIPNV25USU6JRWK=
GCT MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELHeHVKSzVyPUCuN|A3PzJizszN NHPxeY5USU6JRWK=
769-P MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK2TWM2OD1yLkW4OFk6KM7:TR?= NWD3Sng2W0GQR1XS
LOXIMVI MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWToepA1UUN3ME2wMlU5QDN{IN88US=> MWHTRW5ITVJ?
D-336MG NV7SdY5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;qVpBKSzVyPUCuPFQ3OiEQvF2= NX7TUo92W0GQR1XS
S-117 NWP6fpVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BVWhYUUN3ME2wMlkzOTNzIN88US=> NH3YXpZUSU6JRWK=
D-247MG NF24OWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXtTWM2OD1yLkm0PFUzKM7:TR?= NETXUo5USU6JRWK=
TYK-nu NIrq[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTWdoxUUUN3ME2xMlA4QTF{IN88US=> NEnmenJUSU6JRWK=
A498 NY\uXYFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwM{C0Olkh|ryP M1;RbHNCVkeHUh?=
BCPAP NH7lNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP1NFRKSzVyPUGuOlY5QThizszN NGnpWnRUSU6JRWK=
KYSE-180 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\wcY5mUUN3ME2xMlczPzh6IN88US=> Mm\JV2FPT0WU
MIA-PaCa-2 NF\rdo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn1XGRwUUN3ME2xMlc2QTd5IN88US=> MVHTRW5ITVJ?
HCC1395 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnSTWM2OD1zLke4Nlc{KM7:TR?= M3S5N3NCVkeHUh?=
RS4-11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDVPWRKSzVyPUGuPVU1OTVizszN MYTTRW5ITVJ?
NCI-H2122 Mkn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vJZ2lEPTB;Mj6yO|Y5PCEQvF2= NX;acnFPW0GQR1XS
SNU-423 NUnwWZVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJwNEm3PFch|ryP NGDl[FBUSU6JRWK=
SK-LMS-1 NYq5emNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HWXmlEPTB;Mj62OFEzQCEQvF2= MVvTRW5ITVJ?
RPMI-7951 NGK1WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnzTWM2OD1{LkewNVk{KM7:TR?= Ml32V2FPT0WU
COLO-829 M4DmO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHIXnk4UUN3ME2yMlc3PTRizszN NFHmWXFUSU6JRWK=
SCC-9 M{TiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXW[GxKSzVyPUKuPVU1QDVizszN M{frWXNCVkeHUh?=
A704 NYLqPHU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfRbG1nUUN3ME2zMlA5OTJizszN MXPTRW5ITVJ?
HOP-62 M3:wZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTNwM{[wOVQh|ryP NX7NWYxRW0GQR1XS
HCC1569 M4LXTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX1N2JKSzVyPUOuOFg{ODVizszN MX3TRW5ITVJ?
A172 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm4U5FKSzVyPUOuO|U1QThizszN M1\l[XNCVkeHUh?=
MOLT-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHjTWM2OD1|Lki4OVU3KM7:TR?= NXXp[Y1jW0GQR1XS
TE-15 Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTNwOUWzOFMh|ryP MmfsV2FPT0WU
OE19 M{\qXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNwOU[0OVEh|ryP MljmV2FPT0WU
MHH-ES-1 M2X0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{noTmlEPTB;ND6wOFU1PSEQvF2= MkLDV2FPT0WU
NKM-1 NWj5UXZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL5ZWVCUUN3ME20MlE{QTdzIN88US=> M3rqZnNCVkeHUh?=
RCC10RGB NWXkbIQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTOOIVJUUN3ME20MlI6PDd7IN88US=> M{e1N3NCVkeHUh?=
BxPC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTRwN{CzPVEh|ryP NG\YVVdUSU6JRWK=
ALL-PO NEKybWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTRwOEO4OVgh|ryP MVPTRW5ITVJ?
SK-OV-3 MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjYbGxKSzVyPUSuPVk{PCEQvF2= NH:zWppUSU6JRWK=
SW1710 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGToOlFKSzVyPUWuOFI1PTZizszN NVXRfod6W0GQR1XS
NCI-H2452 NXLFZXd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D3VGlEPTB;NT60OVYzQCEQvF2= MWPTRW5ITVJ?
D-392MG MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XnbWlEPTB;NT60PVE1PSEQvF2= NIHrXlhUSU6JRWK=
LB2518-MEL M{LIdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PIVWlEPTB;NT63NlYzPyEQvF2= NHfXNpBUSU6JRWK=
BL-41 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjFcGhKSzVyPUWuPFEzPjZizszN NI\NenBUSU6JRWK=
WM-115 NVfu[FZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHsTWM2OD13LkixOVA6KM7:TR?= MXvTRW5ITVJ?
SK-MEL-2 NFn0ZVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYC2bFloUUN3ME22MlM5OzR2IN88US=> NYSwXXBiW0GQR1XS
CGTH-W-1 M{DObmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzLTWM2OD14LkSxO{DPxE1? MYfTRW5ITVJ?
BB65-RCC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qyNWlEPTB;Nj61N|E6PSEQvF2= M33lTnNCVkeHUh?=
CAL-85-1 NV:5VINIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTZwNkC5N|Yh|ryP MoTlV2FPT0WU
RT-112 M1vTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Di[mlEPTB;Nz6xOlQ2PiEQvF2= M4ftZ3NCVkeHUh?=
MC116 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoCyTWM2OD15LkK4OlkyKM7:TR?= M3HmTHNCVkeHUh?=
G-361 NIPWOYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4qxbWlEPTB;Nz60OlU3OSEQvF2= MmjnV2FPT0WU
SW1417 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTdwNkS1PFQh|ryP M2W5e3NCVkeHUh?=
MV-4-11 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fzOWlEPTB;OD61OFMxPCEQvF2= MlTsV2FPT0WU
CAL-72 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHtTWM2OD16Lke2NVE{KM7:TR?= M3LYNnNCVkeHUh?=
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KARPAS-422 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTd6OT6zNVUh|ryP M2DTSHNCVkeHUh?=
BC-3 Mn7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRThyNT6yNFMh|ryP M3T1c3NCVkeHUh?=
NCI-H1155 NXTpTHhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;tTWM2OD16MUiuNFU6KM7:TR?= NVHJbI96W0GQR1XS
NCI-H1581 NWjVVoVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK1O5BrUUN3ME25NFAvOjNzIN88US=> NY\n[5JxW0GQR1XS

... Click to View More Cell Line Experimental Data

体内研究 CHIR-99021按30 mg/kg 剂量口服处理患2型糖尿病的啮齿类动物模型,增强葡萄糖代谢,处理3-4小时后,最大血浆葡萄糖减少近150 mg/dl,而血浆胰岛素保持或低于对照水平。CHIR-99021按16 或 48 mg/kg剂量口服给药ZDF大鼠,1小时后,再口服葡萄糖,显著改善糖耐量,16 mg/kg 和 48 mg/kg处理组的血浆葡萄糖分别减少14%和33%,较高剂量CHIR-99021处理,再口服葡萄糖,还可以降低高血糖。[1]CHIR-99021处理移植小鼠或人造血干细胞(HSC)的受体小鼠,显著增强造血重建功能,说明GSK-3是一种特异性的HSC活性调节剂。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

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无细胞激酶实验:

聚丙烯96孔板中每孔充满了含27 nM GSK-3α 或 29 nM GSK-3β, 和 0.5 μM 生物素-CREB 肽底物的300 μL 缓冲液 (50 mM Tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM 二硫苏糖醇, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) 。各种浓度CHIR-99021加入3.5 μL DMSO中,随后加入50 μL ATP储存液,使所有无细胞实验中ATP终浓度为1 μM。温育后,100 μL等分试样按一式三份转移至每孔含100 μL 50 μM ATP和 20 mM EDTA的Combiplate 8孔板中。1小时后,使用用PBS将孔洗涤5次,填充200 μL闪烁液,密封,放置30分钟后,然后在闪烁计数器中计数。所有步骤在室温下进行。
细胞实验:

[3]

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  • Cell lines: INS-1E
  • Concentrations: 溶于DMSO, 终浓度为20 μM
  • Incubation Time: 1, 或 4 天
  • Method:

    细胞在饥饿培养基(只含5mM葡萄糖,1%胎牛血清)中维持24小时。然后使用不同浓度的CHIR-99021处理细胞的1天或4天。通过使用CyQuant染料进行细胞DNA染色,测量细胞数,当结合DNA就会发出荧光。温育30分钟后,使用FLUOstar Optima酶标仪测量荧光。通过BrdUrd掺入法测定细胞复制。最后4小时,BrdUrd标记溶液加入到培养基中,然后使用FixDenat溶液固定细胞,与单克隆anti-BrdUrd-POD抗体温育。每孔加入底物溶液后,在微孔板发光检测仪上使用Analyst HT检测系统测量光发射。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 雌性db/db小鼠或雄性2型糖尿病ZDF大鼠
  • Formulation: 在20mM柠檬酸盐缓冲的15%Captisol中配制成溶液,或在0.5%羧甲基纤维素中配制成悬浮液
  • Dosages: ~48 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 93 mg/mL (185.33 mM)
Ethanol 2 mg/mL (3.98 mM)
Water Insoluble
体内 从左到右依次加入纯溶剂:
5% DMSO+30% PEG 300+ddH2O
24mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 501.8
化学式

C22H18Cl2N8.HCl

CAS号 1797989-42-4
稳定性 powder
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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?

  • 回答:

    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.

  • 问题 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?

  • 回答:

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

  • 问题 3:

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

  • 回答:

    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

GSK-3 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID