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73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.

  •  

    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.

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 M4H1UGZ2dmO2aX;uJGF{e2G7 MlXkN{DPxE1? M3\iR|QhcA>? M{jOZ2ROW09? M3\tV2lvcGmkaYTzJJBz\WGmaYDvZ5l1\SCmaX\m[ZJmdnSrYYTpc44> NEPxOI4yOjB3NUKwNC=>
insulin receptor–expressing CHO-IR MWPGeY5kfGmxbjDBd5NigQ>? M1u1O|UxOCCwTR?= NFrLPGc{OCCvaX6= MVXEUXNQ NELXU3NC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= MWexNlYxPjR7Nx?=
H4IIE M1fjUWZ2dmO2aX;uJGF{e2G7 Ml3HNVAh|ryP MUGyOEBp MWHEUXNQ NYTCWodPWmWpdXzheIV{KM7{LXPheIVvcW5iYXP0bZZqfHliYX7kJHRKWkViY3;ueIFqdmmwZzDwdo9ud3SncjDhZ5Rqfmm2eR?= MVGxOVM2ODF7NR?=
Oct4/Sox2/Klf4-infected MEFs MkP2SpVv[3Srb36gRZN{[Xl? NH;2T4EyOCEQvF2= MXyyPEBl NXPMSW5HTE2VTx?= MY\Qdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= M{\lWFE6QDN7MEW1
Sca-1+ HPC Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2CyOVIh|ryP MUm2JIQ> M1SxTWROW09? M{nrZ3N6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG M2LKNlIyPjJ2M{S4
HMC1.2 NGPPcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvDN|Ah|ryP NFqw[mY4OiCq NVftR5lLTE2VTx?= NILBR3BT\WS3Y3XzJINmdGxic4Xyeol3[Wx? NFWwSpczOjB|OUOwNS=>
Endothelial cell(EC) M3vJUGZ2dmO2aX;uJGF{e2G7 NG\VXHU{KM7:TR?= NY[x[YFHTE2VTx?= NV3uOYR[WHKxbX;0[ZMh\W6mb4To[Yxq[WxiY3XscEApTUNrIHTp[oZmemWwdHnheIlwdg>? M1nDSlIzODV{MEC2
PANC1 NXP1e2IzSXCxcITvd4l{KEG|c3H5 NYPjTopUyqB3IN88US=> MlWyO|IhcA>? MX3EUXNQ NWLQZW06XHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn NX7LV2J4OjJ{MEGxPFY>
INS-1E NV3YPWx6TnWwY4Tpc44hSXO|YYm= M4jROFIvPSEQvF2= NXG3bFVoOjRiaB?= Ml;XSG1UVw>? MY\JcoR2[2W|IHGgdoVlfWO2aX;uJI9nKE6SMTDveoVz\XiycnXzd4lwdg>? M3;Jd|IzPDJ5N{C0
hiPSC-NPs NUCwNYxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S5[VPjiIoQvF2= MXK3NkBp NVrjdW92TE2VTx?= NFnON5ZKdmO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vyqB? Mm\iNlI3PDJ4OEe=
platelets MlXLSpVv[3Srb36gRZN{[Xl? NHvHSIEyOCEQvF2= NFPGSpQyPSCvaX6= NFLjVpVFVVOR MV3JcoNz\WG|ZYOgeIhzd22kaX6tcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIFHUVEB{\WO{ZYTpc44> Mn\GNlMzOzl6N{e=
DN3 M1XLUGZ2dmO2aX;uJGF{e2G7 M4ezPVExKM7:TR?= NXe3NoFoQTZiaB?= M2W0e2ROW09? M4PX[Wlv[3KnYYPld{Bk\WyuIHTleoVtd3CvZX70JIFv\CCycn;sbYZmemG2aX;u NE\MV4gzOzV{Nkm4PS=>
embryonic stem cells (ESC) MVzGeY5kfGmxbjDBd5NigQ>? NILkUWY{KML3TR?= MUixNUBl NF\5fJhFVVOR NXPtV45kWHKxbX;0[ZMhe2WuZj3y[Y5mf2GuIH;mJI5iy6:4ZT30fZBmKG2xdYPlJIVu[nK7b37pZ{B{fGWvIHPlcIx{KCiHU1Op M4fwOlI{QDR|M{Gy
H460 M3PNTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO1JOK2VQ>? MVOyOEBp M3K2VWROW09? M4TMT3Bzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> NWXBOpJTOjR|Nke2PFg>
H157 NIjPVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XjTFUhyrWP M1fLVVI1KGh? M3XXTGROW09? M3PoRnBzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> NVPDTIpMOjR|Nke2PFg>
H460 Mn\DRZBweHSxc3nzJGF{e2G7 MWK1JOK2VQ>? MXGyOEBp NHraSFRFVVOR NInvdndCfHSnboXheIV{KGOnbHygZZBweHSxc3nz NIfTW2UzPDN4N{[4PC=>
H157 NHHNWGpCeG:ydH;zbZMhSXO|YYm= M1HMS|UhyrWP NELE[mczPCCq NV74TWJUTE2VTx?= MmjYSI9meyCwb4Sgd4lodmmoaXPhcpRtgSCjZn\lZ5Qh[XCxcITvd4l{ NF7N[Y0zPDN4N{[4PC=>
A549 MXnBdI9xfG:|aYOgRZN{[Xl? NXf6ZXppPSEEtV2= MX:yOEBp MXPEUXNQ M1PQeWlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= MVOyOFM3PzZ6OB?=
Neural progenitor cells NI[0[VdHfW6ldHnvckBCe3OjeR?= MnrwN{DPxE1? NEfhRWkyOCCm MYPEUXNQ NFzodlRKdmS3Y3XzJIdmdmW{YYTpc44hd2ZibnX1doFtKHC{b3flcol1d3JiY3XscJM> MUGyOFY{QDB|NB?=
ES-D3 M4fDbGN6fG:2b4jpZ{BCe3OjeR?= NFjsSoUyOMLizszN M{\5bFMh\A>? NEnjdJpFVVOR M13CW2lv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP M3LtXVI1Pzd7M{[1
ES-CCE NGHXcoFEgXSxdH;4bYMhSXO|YYm= NEDZTGoyOMLizszN NUnwbolLOyCm MkS1SG1UVw>? MUXJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fS=> M1Ha[FI1Pzd7M{[1
ES-D3 NWLxbIhjTnWwY4Tpc44hSXO|YYm= M{fVOVXDqM7:TR?= NXXIPHFlOyCm NXLkOXc1TE2VTx?= M3nvTXN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? Mn34NlQ4Pzl|NkW=
ES-CCE NVfFZm9iTnWwY4Tpc44hSXO|YYm= NF7CV3I2yqEQvF2= M4jSOlMh\A>? MmS1SG1UVw>? MlizV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 NY\SXGJkOjR5N{mzOlU>
SW982 M3vhc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofOTWM2OD1yLkKxOFE3KM7:TR?= M{HrU3NCVkeHUh?=
GCT MmPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[zSlQ5UUN3ME2wMlMxPjd{IN88US=> M2HS[nNCVkeHUh?=
769-P MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHTXFRKSzVyPUCuOVg1QTlizszN NIntemFUSU6JRWK=
LOXIMVI MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrPO2NRUUN3ME2wMlU5QDN{IN88US=> NUC5[GhsW0GQR1XS
D-336MG NWmzVmh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrQR49KSzVyPUCuPFQ3OiEQvF2= NIL0bWFUSU6JRWK=
S-117 M3zNUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwOUKxN|Eh|ryP NFP4S|NUSU6JRWK=
D-247MG M1G4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPFTWM2OD1yLkm0PFUzKM7:TR?= MnfCV2FPT0WU
TYK-nu NYXNSIM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13yRWlEPTB;MT6wO|kyOiEQvF2= M4nPTHNCVkeHUh?=
A498 M1;te2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWWwXGdIUUN3ME2xMlMxPDZ7IN88US=> NVzrXpR2W0GQR1XS
BCPAP NWDoTGJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwNk[4PVgh|ryP MmTUV2FPT0WU
KYSE-180 NWHOUFUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFwN{K3PFgh|ryP M2DIRnNCVkeHUh?=
MIA-PaCa-2 NIDKO4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfuWlJKSzVyPUGuO|U6PzdizszN NIXVdY1USU6JRWK=
HCC1395 M4PjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIn1cGVKSzVyPUGuO|gzPzNizszN MmrEV2FPT0WU
RS4-11 NGjJNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwOUW0NVUh|ryP Mmj6V2FPT0WU
NCI-H2122 NYLUcGdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX72bJRbUUN3ME2yMlI4Pjh2IN88US=> M1zaO3NCVkeHUh?=
SNU-423 M3H5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHz3ZW9KSzVyPUKuOFk4QDdizszN NFXEe|VUSU6JRWK=
SK-LMS-1 NX\BbIltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHLTWM2OD1{Lk[0NVI5KM7:TR?= M1zvR3NCVkeHUh?=
RPMI-7951 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fFXGlEPTB;Mj63NFE6OyEQvF2= NHvMUopUSU6JRWK=
COLO-829 NGLPbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJwN{[1OEDPxE1? MW\TRW5ITVJ?
SCC-9 NE\GcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGezenlKSzVyPUKuPVU1QDVizszN NGXQOmZUSU6JRWK=
A704 NGi1bXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPkTWM2OD1|LkC4NVIh|ryP NI\CTlBUSU6JRWK=
HOP-62 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITvXXhKSzVyPUOuN|YxPTRizszN MVjTRW5ITVJ?
HCC1569 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTNwNEizNFUh|ryP MoPSV2FPT0WU
A172 NVjsN5I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljGTWM2OD1|Lke1OFk5KM7:TR?= MlrXV2FPT0WU
MOLT-16 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHuTWM2OD1|Lki4OVU3KM7:TR?= MlPEV2FPT0WU
TE-15 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF23[XFKSzVyPUOuPVU{PDNizszN MlnBV2FPT0WU
OE19 NFmwRXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrLSoN3UUN3ME2zMlk3PDVzIN88US=> NWPQemhIW0GQR1XS
MHH-ES-1 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3S2d2lEPTB;ND6wOFU1PSEQvF2= NVyzWYNbW0GQR1XS
NKM-1 MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MniyTWM2OD12LkGzPVcyKM7:TR?= M4\sT3NCVkeHUh?=
RCC10RGB Ml:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PQNGlEPTB;ND6yPVQ4QSEQvF2= MlKyV2FPT0WU
BxPC-3 NXPROoJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Dk[2lEPTB;ND63NFM6OSEQvF2= MUjTRW5ITVJ?
ALL-PO MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHHO|NbUUN3ME20Mlg{QDV6IN88US=> NImxN|ZUSU6JRWK=
SK-OV-3 NUPvXW9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLifVhKSzVyPUSuPVk{PCEQvF2= M{\Qd3NCVkeHUh?=
SW1710 MnH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXQUnFNUUN3ME21MlQzPDV4IN88US=> MoHIV2FPT0WU
NCI-H2452 MknVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX4Uog5UUN3ME21MlQ2PjJ6IN88US=> MVHTRW5ITVJ?
D-392MG NGDxeIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTVwNEmxOFUh|ryP MoroV2FPT0WU
LB2518-MEL NYD6VHJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LWe2lEPTB;NT63NlYzPyEQvF2= MkPQV2FPT0WU
BL-41 NGfSeGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHCToZKSzVyPUWuPFEzPjZizszN NITNd2NUSU6JRWK=
WM-115 NFXMWVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm2TGhkUUN3ME21MlgyPTB7IN88US=> M4XZWnNCVkeHUh?=
SK-MEL-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu2TWM2OD14LkO4N|Q1KM7:TR?= NEfLcG9USU6JRWK=
CGTH-W-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorsTWM2OD14LkSxO{DPxE1? M3z5ZXNCVkeHUh?=
BB65-RCC M2TJPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTKWHVTUUN3ME22MlU{OTl3IN88US=> M4DDeXNCVkeHUh?=
CAL-85-1 NUfSbpp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTZwNkC5N|Yh|ryP MlXNV2FPT0WU
RT-112 NIjEfI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnWe4ZKSzVyPUeuNVY1PTZizszN MUjTRW5ITVJ?
MC116 M2DCV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTdwMki2PVEh|ryP MXLTRW5ITVJ?
G-361 NEPMSo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTdwNE[1OlEh|ryP M2\kTHNCVkeHUh?=
SW1417 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj2[|ZKSzVyPUeuOlQ2QDRizszN MUjTRW5ITVJ?
MV-4-11 NIP0dnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HKZmlEPTB;OD61OFMxPCEQvF2= M1zkOnNCVkeHUh?=
CAL-72 M1L5Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRThwN{[xNVMh|ryP NHSwfVhUSU6JRWK=
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NOS-1 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;YSmlEPTB;MUO0Mlc3PSEQvF2= NHnxd5FUSU6JRWK=
G-402 NGTwNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPjWGpKSzVyPUGzOU4zQTVizszN NIHvN5FUSU6JRWK=
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OVCAR-4 M3LqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTF2MD63OFkh|ryP MYLTRW5ITVJ?
Detroit562 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X2O2lEPTB;MUSxMlQ3PiEQvF2= M2fpS3NCVkeHUh?=
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NCI-H810 MkjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\IOIMyUUN3ME2xOFMvPjh5IN88US=> M3WwSHNCVkeHUh?=
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GCIY MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLsc2lTUUN3ME2xOFcvPzl5IN88US=> MV7TRW5ITVJ?
GAMG NXjQdXVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXITWM2OD1zNEiuNlQ4KM7:TR?= M3LiV3NCVkeHUh?=
KYSE-520 M3rzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF2OD61OEDPxE1? MkfUV2FPT0WU
LB647-SCLC NHXIdnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF2OD61OlIh|ryP NWjFUmxUW0GQR1XS
639-V NYfGN|hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjTN5V7UUN3ME2xOFgvPzB3IN88US=> MlP3V2FPT0WU
TE-9 NFW3cHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonDTWM2OD1zNEmuOFQ{KM7:TR?= MoHhV2FPT0WU
Caov-3 NFnNO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDOPZNKSzVyPUG0PU44OTRizszN NXHFNYhKW0GQR1XS
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NCI-H748 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvRXlNKSzVyPUG1NE4zODlizszN NGLuS4lUSU6JRWK=
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GAK MlLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYKwXXBXUUN3ME2xOVEvOzd2IN88US=> MXzTRW5ITVJ?
AsPC-1 M4T4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj4cYlrUUN3ME2xOVIvPzZ2IN88US=> M3TkSXNCVkeHUh?=
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TT MnWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvCXmJEUUN3ME2xOVMvPDlizszN M3LjNHNCVkeHUh?=
Calu-1 M4faNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mli2TWM2OD1zNUSuNFA{KM7:TR?= NWPQOXR4W0GQR1XS
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DK-MG NV7oTHU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DyRWlEPTB;MUW1MlE5OyEQvF2= NFixTZRUSU6JRWK=
CAL-120 M1PNSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XpRWlEPTB;MUW1MlgzOSEQvF2= M3Ls[3NCVkeHUh?=
HCC1419 M3Xlfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmn5TWM2OD1zNU[uNFc4KM7:TR?= Mmq4V2FPT0WU
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HCC38 NV;VXHJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjnVYNKSzVyPUG1O{4{PjlizszN Mn72V2FPT0WU
HCC70 NXPVTZVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPlV3N{UUN3ME2xOVkvOjR{IN88US=> M{Hx[XNCVkeHUh?=
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NCI-H2052 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfnVGpIUUN3ME2xOVkvPTh|IN88US=> Ml;DV2FPT0WU
EFO-27 MmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHYTWM2OD1zNkCuOVg1KM7:TR?= NXjsfmc4W0GQR1XS
CAL-62 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLEVm1OUUN3ME2xOlIvPjF|IN88US=> MVvTRW5ITVJ?
CHP-212 NF7Xe4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[1TWM2OD1zNkOuOlI3KM7:TR?= NYnYeGM2W0GQR1XS
AU565 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF4Mz62OEDPxE1? MoXLV2FPT0WU
Ca9-22 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jPOGlEPTB;MU[0MlMzOSEQvF2= Mk\1V2FPT0WU
EFO-21 MoeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfZTWM2OD1zNkWuOFUh|ryP NXK2N4s1W0GQR1XS
KINGS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF4Nz6zOVQh|ryP Mn7SV2FPT0WU
JVM-2 MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGmzdnBKSzVyPUG2O{41PTFizszN NWjZRXcyW0GQR1XS
OVCAR-5 M1:zZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrZTWM2OD1zNkiuN|A6KM7:TR?= M3;0enNCVkeHUh?=
Calu-3 NF3mbnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTUTWM2OD1zNkiuN|EyKM7:TR?= NGqzWGtUSU6JRWK=
CP66-MEL MlfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PyW2lEPTB;MU[4MlQyPSEQvF2= Mk\aV2FPT0WU
KYSE-150 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrQTWM2OD1zNkmuOlM3KM7:TR?= NEC4WVhUSU6JRWK=
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SW620 MnrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWmwWHJvUUN3ME2xO|EvPTN3IN88US=> Ml;tV2FPT0WU
HuO-3N1 NWO4NHFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG4RWtLUUN3ME2xO|IvOjd|IN88US=> NWTqWHVrW0GQR1XS
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ME-180 NUPO[WpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHTV3dKSzVyPUG3OE4xOTZizszN MXvTRW5ITVJ?
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COLO-741 Mm\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3WTWM2OD1zN{euOVYyKM7:TR?= M1HQOnNCVkeHUh?=
SK-NEP-1 NFzCRoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6wPIx3UUN3ME2xO|cvQDB4IN88US=> NWHSbWNkW0GQR1XS
NB10 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3X4O2lEPTB;MUe3Mlg1PiEQvF2= M{PNW3NCVkeHUh?=
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NCI-H522 M3;NRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PWXmlEPTB;MUixMlA2QSEQvF2= NHfYbHRUSU6JRWK=
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GI-ME-N MnX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XSZ2lEPTB;MUixMlY4OiEQvF2= MUjTRW5ITVJ?
SBC-5 NYTmZmFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\OTJBmUUN3ME2xPFEvQTN2IN88US=> M17tbHNCVkeHUh?=
ONS-76 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO4[mlCUUN3ME2xPFIvOzh5IN88US=> NYHYd2tiW0GQR1XS
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LB2241-RCC MkDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\m[IdKSzVyPUG4OU4yPDVizszN MUTTRW5ITVJ?
NCI-H1563 M4nKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF6NT6yNFkh|ryP M3jsOnNCVkeHUh?=
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MONO-MAC-6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jFe2lEPTB;MUi3MlM6OiEQvF2= NFfvS3dUSU6JRWK=
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SK-LU-1 NWnYdIFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfnTHF4UUN3ME2xPFgvPDJ6IN88US=> MmXLV2FPT0WU
NCI-H1299 NF:zSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfqTWM2OD1zOEiuO|E6KM7:TR?= M4LEWnNCVkeHUh?=
KG-1 NVnYSHdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Sx[2lEPTB;MUi5Mlc6QCEQvF2= NIfWPYRUSU6JRWK=
ETK-1 M4rIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof6TWM2OD1zOUCuNVgyKM7:TR?= MU\TRW5ITVJ?
NCI-H838 NUjyUHF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF7MD6zOEDPxE1? M4DpTnNCVkeHUh?=
HCE-4 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PFNmlEPTB;MUmwMlk6OiEQvF2= NGLYPI1USU6JRWK=
A2780 NX3qcGJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\0dWlEPTB;MUmyMlg6OSEQvF2= MmP3V2FPT0WU
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HGC-27 MkXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP4TWM2OD1zOUWuOVM5KM7:TR?= MnO0V2FPT0WU
SW1088 M3Gxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWwTWM2OD1zOUWuOlc4KM7:TR?= MY\TRW5ITVJ?
KOSC-2 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\DTWM2OD1zOUWuPFE5KM7:TR?= NGn5bGRUSU6JRWK=
TE-1 Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\QVYZVUUN3ME2xPVYvOjZizszN MV\TRW5ITVJ?
SW780 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vJcWlEPTB;MUm2Mlc{PCEQvF2= M4LoTnNCVkeHUh?=
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IA-LM NYCwdphGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3uTWM2OD1zOUeuPFIzKM7:TR?= MmPLV2FPT0WU
TE-5 NVvkc3JET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL3Z|N[UUN3ME2xPVgvODN|IN88US=> NXvLS4lkW0GQR1XS
JVM-3 NYHBcWZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvIdVJjUUN3ME2xPVgvPDF7IN88US=> NIPhSIhUSU6JRWK=
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QIMR-WIL NV7lZW5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mny3TWM2OD1{MECuNVE3KM7:TR?= M{XDV3NCVkeHUh?=
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BC-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRThyNT6yNFMh|ryP M1uwOXNCVkeHUh?=
NCI-H1155 M3WxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0TWM2OD16MUiuNFU6KM7:TR?= MofTV2FPT0WU
NCI-H1581 NGXZc4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LrRmlEPTB;OUCwMlI{OSEQvF2= NVv0VGZHW0GQR1XS

... 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]
+ 展开

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 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
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
in solvent
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.

Selleck产品目录册

GSK-3 Signaling Pathway Map

GSK-3 Inhibitors with Unique Features

  • 选择性强的GSK-3抑制剂

    TWS119 : GSK-3β-selective, IC50 of 30 nM.

  • 活性最高的GSK-3抑制剂

    CHIR-98014 : GSK-3α, IC50=0.65 nM; GSK-3β, IC50=0.58 nM.

  • 用于临床的GSK-3抑制剂

    Tideglusib : Phase II for Alzheimer's disease.

  • 最新的GSK-3抑制剂

    AZD1080 : Orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively.

相关GSK-3产品

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂， IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性，对GSK-3β的选择性是对CDKs选择性的350倍。

  • LY2090314 New

    LY2090314是一种有效的GSK-3抑制剂，作用于GSK-3α/β，IC50为1.5 nM/0.9 nM；可提高以铂类为基础的化疗方案的疗效。LY2090314对GSK3具有高选择性，对其他大多数激酶的抑制活性低。

  • TDZD-8 New

    TDZD-8是一种非ATP竞争性GSK-3β抑制剂，IC50为2 μM；对CDK1， casein kinase II， PKA和PKC具有最低限度的抑制效果。

  • TWS119

    TWS119是一种GSK-3β抑制剂，在无细胞试验中IC50为30 nM；能够诱导神经细胞的分化，并且有助于干细胞生物学的研究。

  • SB216763

    SB216763是一种有效的，选择性GSK-3α抑制剂，IC50为34.3 nM；对GSK-3β具有同样的抑制作用。

  • Tideglusib

    Tideglusib是一种不可逆的，非ATP竞争性的GSK-3β抑制剂，无细胞试验中IC50为60 nM，不能抑制位于活性位点的同源于 Cys-199的 Cys激酶。Phase 2。

  • CHIR-98014

    CHIR-98014是一种有效的GSK-3α/β抑制剂，无细胞试验中IC50为0.65 nM/0.58 nM，作用于GSK-3比作用于其最密切的同源物Cdc2 和 ERK2选择性高。

  • BIO

    BIO是一种特异性的GSK-3抑制剂，无细胞试验中作用于GSK-3α/β的IC50为5 nM，比作用于CDK5选择性高16倍以上，也是一种泛JAK抑制剂。

    Features:BIO是第一个维持人类和小鼠的胚胎干细胞自我更新的药理剂。

  • AR-A014418

    AR-A014418是一种ATP竞争性和选择性的GSK3β抑制剂，无细胞试验中IC50和Ki为104 nM和38 nM，而对被测试的其他26种激酶没有显著抑制作用。

  • IM-12

    IM-12是一种选择性的GSK-3β抑制剂,其IC50为53 nM，增强了Wnt信号通路。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID