CHIR-99021 (CT99021) HCl

For research use only. Not for use in humans.

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  
10mM (1mL in DMSO) RMB 2780.99 现货
RMB 733.53 现货
RMB 1373.92 现货
RMB 4650.09 现货
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客户使用Selleck生产的CHIR-99021 (CT99021) HCl发表文献130篇:

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 NYnsPYhVTnWwY4Tpc44hSXO|YYm= NEW5WIs{KM7:TR?= NEX2fm41KGh? MVPEUXNQ MmC2TY5pcWKrdIOgdJJm[WSrcH;jfZRmKGSrZn\ldoVvfGmjdHnvci=> NFXjVW0yOjB3NUKwNC=>
insulin receptor–expressing CHO-IR MVPGeY5kfGmxbjDBd5NigQ>? MVm1NFAhdk1? NVTzWYZ[OzBibXnu MXPEUXNQ NFzRZ5JC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= MVuxNlYxPjR7Nx?=
H4IIE NGfld5hHfW6ldHnvckBCe3OjeR?= MVqxNEDPxE1? NXj5RnJiOjRiaB?= NVjlNVFxTE2VTx?= NU\NUY9VWmWpdXzheIV{KM7{LXPheIVvcW5iYXP0bZZqfHliYX7kJHRKWkViY3;ueIFqdmmwZzDwdo9ud3SncjDhZ5Rqfmm2eR?= MUmxOVM2ODF7NR?=
Oct4/Sox2/Klf4-infected MEFs MWfGeY5kfGmxbjDBd5NigQ>? NF7wO5UyOCEQvF2= M3vZNlI5KGR? NF7qPIVFVVOR M2nsTXBzd22xdHXzJG1GTnNicnXwdo9oemGvbXnu[{BVemGwc3T1Z4VlKGK7IF;jeFQtKFOxeEKsJIFv\CCNbH[0 NVW4SVJUOTl6M{mwOVU>
Sca-1+ HPC Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr6PWszKM7:TR?= MVW2JIQ> M{izOGROW09? MmHNV5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= Mnm5NlE3OjR|NEi=
HMC1.2 NFrTeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXnN|Ah|ryP NVGy[GVJPzJiaB?= MlPxSG1UVw>? NV30cJJNWmWmdXPld{Bk\WyuIIP1dpZqfmGu MmLiNlIxOzl|MEG=
Endothelial cell(EC) NVr5TY92TnWwY4Tpc44hSXO|YYm= M3XXNFMh|ryP M1XjVmROW09? M2\3V3Bzd22xdHXzJIVv\G:2aHXsbYFtKGOnbHygLGVEMSCmaX\m[ZJmdnSrYYTpc44> NV32cGtIOjJyNUKwNFY>
PANC1 MVLBdI9xfG:|aYOgRZN{[Xl? MUpCpFUh|ryP NIPOcZk4OiCq M4fNPGROW09? M{jxdnRzcWepZYLzJIFvKGGyb4D0c5Rq[yC{ZYPwc45{\Q>? M1fhPVIzOjBzMUi2
INS-1E NGfi[mxHfW6ldHnvckBCe3OjeR?= NXqx[4NVOi53IN88US=> NV7zUYpzOjRiaB?= NIPDVYdFVVOR NFrINWJKdmS3Y3XzJIEhemWmdXP0bY9vKG:oIF7QNUBwfmW{ZYjwdoV{e2mxbh?= NXHnOHczOjJ2Mke3NFQ>
hiPSC-NPs NXfMNHVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H3d|PjiIoQvF2= NIryfJU4OiCq M4rIVmROW09? MoTsTY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh NV3wb5F[OjJ4NEK2PFc>
platelets NV:1PIl6TnWwY4Tpc44hSXO|YYm= NH3hbHIyOCEQvF2= M1HadlE2KG2rbh?= Ml\sSG1UVw>? MnjFTY5kemWjc3XzJJRpem:vYnnuMY1m\GmjdHXkJJBt[XSnbHX0JIFo\3KnZ3H0bY9vKGGwZDDBWHAhe2WlcnX0bY9v MWiyN|I{QTh5Nx?=
DN3 MX3GeY5kfGmxbjDBd5NigQ>? MWKxNEDPxE1? M{HweFk3KGh? M1j1VmROW09? MXnJcoNz\WG|ZYOgZ4VtdCCmZY\lcI9xdWWwdDDhcoQheHKxbHnm[ZJifGmxbh?= M3jzUFI{PTJ4OUi5
embryonic stem cells (ESC) MkD2SpVv[3Srb36gRZN{[Xl? NIjyOnM{KML3TR?= NI\qVGkyOSCm M4L4fGROW09? NYnSTWVlWHKxbX;0[ZMhe2WuZj3y[Y5mf2GuIH;mJI5iy6:4ZT30fZBmKG2xdYPlJIVu[nK7b37pZ{B{fGWvIHPlcIx{KCiHU1Op MoTkNlM5PDN|MUK=
H460 NF\4OZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Pqb|UhyrWP NYrmWFVuOjRiaB?= NVrVZ2gxTE2VTx?= NVf3RoJVWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v MkPWNlQ{Pjd4OEi=
H157 M4CyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojUOUDDvU1? MkPGNlQhcA>? NGrX[mVFVVOR M{XpVXBzd22xdHXzJINmdGxicILvcIln\XKjdHnvci=> MWiyOFM3PzZ6OB?=
H460 M2PPO2Fxd3C2b4Ppd{BCe3OjeR?= MmHzOUDDvU1? M4jwblI1KGh? NFLXeYNFVVOR NX7jOJk5SXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> MV:yOFM3PzZ6OB?=
H157 MULBdI9xfG:|aYOgRZN{[Xl? NH[4OGs2KML3TR?= M3LFdlI1KGh? NWHremc2TE2VTx?= M3ntNGRw\XNibn;0JJNq\26rZnnjZY51dHliYX\m[YN1KGGyb4D0c5Nqew>? NFzzeW0zPDN4N{[4PC=>
A549 NXXzfWNNSXCxcITvd4l{KEG|c3H5 MmrLOUDDvU1? NX:2U4NQOjRiaB?= NXrZd4FjTE2VTx?= MWfJcoNz\WG|ZYOgZ4VtdCCjcH;weI9{cXN? MmjRNlQ{Pjd4OEi=
Neural progenitor cells MnyySpVv[3Srb36gRZN{[Xl? NHj3dnk{KM7:TR?= NUnQcYV4OTBiZB?= NXrZTnV6TE2VTx?= NXrQWpp1UW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ M1LRXFI1PjN6MEO0
ES-D3 MmnrR5l1d3SxeHnjJGF{e2G7 MXWxNOKh|ryP MWKzJIQ> MmjWSG1UVw>? MkW1TY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJkhf2m2aDDJR|UxKG:oIESuPUDPxE1? M2j0flI1Pzd7M{[1
ES-CCE NUW5Z5hXS3m2b4TvfIlkKEG|c3H5 Moi2NVDDqM7:TR?= NFX5SYM{KGR? MlvJSG1UVw>? MkTHTY5lfWOnczDtc4RmemG2ZTDjfZRwfG:6aXPpeJk> MUeyOFc4QTN4NR?=
ES-D3 NXexSlI5TnWwY4Tpc44hSXO|YYm= M3;xfFXDqM7:TR?= NIP5NVY{KGR? M3m3TmROW09? NUe2UHBvW3S{b37ncJkhcW6mdXPld{B1cGViYXP0bZZqfHlib3[gW451N2KndHGtZ4F1\W6rbjDwZZRpf2G7 NFXSWYkzPDd5OUO2OS=>
ES-CCE M1PLTmZ2dmO2aX;uJGF{e2G7 NI\YRpA2yqEQvF2= MlzMN{Bl MUDEUXNQ MoDEV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 MWWyOFc4QTN4NR?=
SW982 M17aNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHsdXVKSzVyPUCuNlE1OTZizszN MmDGV2FPT0WU
GCT NY\vXoQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvsO4hrUUN3ME2wMlMxPjd{IN88US=> MUPTRW5ITVJ?
769-P NGq3fVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDGTWM2OD1yLkW4OFk6KM7:TR?= Mn2xV2FPT0WU
LOXIMVI MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLPbY5NUUN3ME2wMlU5QDN{IN88US=> NWS5XnhXW0GQR1XS
D-336MG MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3LSoJKSzVyPUCuPFQ3OiEQvF2= MVvTRW5ITVJ?
S-117 NGrZOI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zxe2lEPTB;MD65NlE{OSEQvF2= M3zCXHNCVkeHUh?=
D-247MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:wW4hoUUN3ME2wMlk1QDV{IN88US=> MV\TRW5ITVJ?
TYK-nu NVTSflFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjyTHZFUUN3ME2xMlA4QTF{IN88US=> NVHnbo9MW0GQR1XS
A498 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPE[nNsUUN3ME2xMlMxPDZ7IN88US=> NEDoVnVUSU6JRWK=
BCPAP NXT4eVF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTKTWM2OD1zLk[2PFk5KM7:TR?= Mn3pV2FPT0WU
KYSE-180 M3XS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\pemNkUUN3ME2xMlczPzh6IN88US=> NVKxXpdYW0GQR1XS
MIA-PaCa-2 NHf1d5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLV[VFKSzVyPUGuO|U6PzdizszN NFTXflBUSU6JRWK=
HCC1395 NFX1TFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWxTWM2OD1zLke4Nlc{KM7:TR?= MmfrV2FPT0WU
RS4-11 MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPITWM2OD1zLkm1OFE2KM7:TR?= NVfLbGNGW0GQR1XS
NCI-H2122 M3:1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljFTWM2OD1{LkK3Olg1KM7:TR?= M3\RN3NCVkeHUh?=
SNU-423 M4\1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\yTWM2OD1{LkS5O|g4KM7:TR?= NXrvfm5rW0GQR1XS
SK-LMS-1 NHnOemRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELoSm1KSzVyPUKuOlQyOjhizszN NXvOdFdsW0GQR1XS
RPMI-7951 NHXwXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfKe2NKSzVyPUKuO|AyQTNizszN NXPYOnJ[W0GQR1XS
COLO-829 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDqOWFRUUN3ME2yMlc3PTRizszN M3jWNnNCVkeHUh?=
SCC-9 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5RmlEPTB;Mj65OVQ5PSEQvF2= Moj5V2FPT0WU
A704 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIO3W3BKSzVyPUOuNFgyOiEQvF2= NYrhSYZMW0GQR1XS
HOP-62 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjRbm9pUUN3ME2zMlM3ODV2IN88US=> MUjTRW5ITVJ?
HCC1569 M2TpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNwNEizNFUh|ryP M{PtVHNCVkeHUh?=
A172 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEGwdXFKSzVyPUOuO|U1QThizszN NFvQVlZUSU6JRWK=
MOLT-16 MmfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNwOEi1OVYh|ryP MVrTRW5ITVJ?
TE-15 NVjsbY96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNwOUWzOFMh|ryP NYf4SldLW0GQR1XS
OE19 M2nRO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTNwOU[0OVEh|ryP NHzDZWVUSU6JRWK=
MHH-ES-1 MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOwSG8{UUN3ME20MlA1PTR3IN88US=> NFLEV4xUSU6JRWK=
NKM-1 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrTc2gzUUN3ME20MlE{QTdzIN88US=> NVzEem1QW0GQR1XS
RCC10RGB MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTRwMkm0O|kh|ryP NEXmTJJUSU6JRWK=
BxPC-3 M4LHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nWPGlEPTB;ND63NFM6OSEQvF2= MWfTRW5ITVJ?
ALL-PO NUHFNpBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j0WmlEPTB;ND64N|g2QCEQvF2= NF7ufGZUSU6JRWK=
SK-OV-3 NY\R[Zh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz3RpdKSzVyPUSuPVk{PCEQvF2= M{f6e3NCVkeHUh?=
SW1710 MmCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nEV2lEPTB;NT60NlQ2PiEQvF2= M3O5N3NCVkeHUh?=
NCI-H2452 NGjtfXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\xTWM2OD13LkS1OlI5KM7:TR?= M4C3cXNCVkeHUh?=
D-392MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq5W3FKSzVyPUWuOFkyPDVizszN NV3QcXJFW0GQR1XS
LB2518-MEL M3;2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLnUmNuUUN3ME21MlczPjJ5IN88US=> MX3TRW5ITVJ?
BL-41 M120dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTVwOEGyOlYh|ryP MUnTRW5ITVJ?
WM-115 NYjXWpZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jIZmlEPTB;NT64NVUxQSEQvF2= M{L2cHNCVkeHUh?=
SK-MEL-2 NFnSTVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LwcWlEPTB;Nj6zPFM1PCEQvF2= M3faSHNCVkeHUh?=
CGTH-W-1 NUnPcFJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TrfWlEPTB;Nj60NVch|ryP M3rmenNCVkeHUh?=
BB65-RCC M1L2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH2NGtsUUN3ME22MlU{OTl3IN88US=> MkK0V2FPT0WU
CAL-85-1 Mn[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInKUo1KSzVyPU[uOlA6OzZizszN MUTTRW5ITVJ?
RT-112 M{HSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2wTWM2OD15LkG2OFU3KM7:TR?= M1[2S3NCVkeHUh?=
MC116 NUHXcllMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXXZphKSzVyPUeuNlg3QTFizszN MoG2V2FPT0WU
G-361 NWPmZnF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT0c2hKSzVyPUeuOFY2PjFizszN MYPTRW5ITVJ?
SW1417 M3XvSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j6TWlEPTB;Nz62OFU5PCEQvF2= MUjTRW5ITVJ?
MV-4-11 M1WyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRThwNUSzNFQh|ryP MVTTRW5ITVJ?
CAL-72 NXLQ[JpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRThwN{[xNVMh|ryP NFPZXYRUSU6JRWK=
MKN28 NEP2UGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nSc2lEPTB;OD64PFUyPiEQvF2= NXfDSXd[W0GQR1XS
MEG-01 NGPIUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXaTWM2OD16Lkm5NFQ{KM7:TR?= NEXmfYdUSU6JRWK=
ACHN MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vJeWlEPTB;OT6zNFU1PiEQvF2= NWr5V2JEW0GQR1XS
NCI-H1755 M4DpW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2yTWM2OD17LkO5PVg3KM7:TR?= NYXpNIlSW0GQR1XS
NCI-H64 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ruS2lEPTB;OT60NlI2PSEQvF2= NH\4UmlUSU6JRWK=
COLO-205 MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTlwNEO4NlEh|ryP MkDNV2FPT0WU
CTV-1 NIK4eWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\hW2lEPTB;OT60N|g6PCEQvF2= NGfmSWhUSU6JRWK=
U-2-OS MnyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljUTWM2OD17LkS1NFA3KM7:TR?= Ml[xV2FPT0WU
LB996-RCC NWnrc2FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\TUndKSzVyPUmuOVI{QTdizszN NGrMTXFUSU6JRWK=
SK-N-DZ MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1O0VGlEPTB;OT62OVc1OiEQvF2= MXTTRW5ITVJ?
EFM-19 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTKTWM2OD17Lke1OVY3KM7:TR?= MULTRW5ITVJ?
DBTRG-05MG MnyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHOZ45yUUN3ME25Mlc4PzdizszN NXPKSY83W0GQR1XS
U-118-MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nnbmlEPTB;OT65OFQ1PCEQvF2= NVTWco0zW0GQR1XS
LB1047-RCC MmSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTlwOUm3PVgh|ryP M1WzWXNCVkeHUh?=
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NOS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTF|ND63OlUh|ryP NVryRo01W0GQR1XS
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BHT-101 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLmTpVbUUN3ME2xOFAvOjB6IN88US=> NUDGcoV{W0GQR1XS
OVCAR-4 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKxTWM2OD1zNECuO|Q6KM7:TR?= MkPqV2FPT0WU
Detroit562 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXK4UpRPUUN3ME2xOFEvPDZ4IN88US=> NIHQWo5USU6JRWK=
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LB647-SCLC MoTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\4WZVOUUN3ME2xOFgvPTZ{IN88US=> M3TYSXNCVkeHUh?=
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DG-75 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ZVFl7UUN3ME2xOVYvPjl2IN88US=> M{PwbnNCVkeHUh?=
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NCI-H2052 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiwTWM2OD1zNUmuOVg{KM7:TR?= NYHBNphkW0GQR1XS
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CAL-62 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f1VWlEPTB;MU[yMlYyOyEQvF2= MYDTRW5ITVJ?
CHP-212 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLjPGNFUUN3ME2xOlMvPjJ4IN88US=> MlK1V2FPT0WU
AU565 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHJT5FLUUN3ME2xOlMvPjRizszN MYPTRW5ITVJ?
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JVM-2 MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLLTWM2OD1zNkeuOFUyKM7:TR?= MmS5V2FPT0WU
OVCAR-5 MmnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\vS5lKSzVyPUG2PE4{ODlizszN MWHTRW5ITVJ?
Calu-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jzN2lEPTB;MU[4MlMyOSEQvF2= M3\tT3NCVkeHUh?=
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KYSE-150 MorSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7vWVVjUUN3ME2xOlkvPjN4IN88US=> M4ntNnNCVkeHUh?=
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SW756 M3y3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\sXWVOUUN3ME2xO|QvQDZ|IN88US=> MmfRV2FPT0WU
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LB2241-RCC M2LCd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O5eGlEPTB;MUi1MlE1PSEQvF2= NEfGbVBUSU6JRWK=
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KYSE-70 NV\E[VF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[zTWM2OD1{MEOuPFc6KM7:TR?= NGjMXo5USU6JRWK=
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NCI-H1651 NVLEdJlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJyNj63N{DPxE1? Mnq1V2FPT0WU
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DJM-1 M4fuSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7Hc4VCUUN3ME2yNFkvQDl5IN88US=> MkDnV2FPT0WU
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EW-18 Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr5TWM2OD1{MUCuO|Y{KM7:TR?= MWPTRW5ITVJ?
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin; 

PubMed: 30709379     


NCI-H460 cells were co-cultured with HUVECs in a 3D culture system, and then treated with 1 μM CHIR-99021, 10 μM or 20 μM Cisplatin, or a combination of both, for 24 h. Cells were harvested and immunoblotted with anti-cleaved PARP, anti-CD31, anti-VE-cadherin, anti-α-SMA, anti-vimentin, and anti-β-actin antibodies. 

CTNNB1; 

PubMed: 23993102     


Treatment with the GSK3β inhibitor CHIR-99021 led to increased levels of β-catenin in RKO and HT29 (non-mutant) cells.

β-catenin; 

PubMed: 24165128     


HeLa cells were treated with 5 μm CHIR-99021 for the indicated times. The samples were analyzed by Western blot.

30709379 23993102 24165128
Growth inhibition assay
Cell viability; 

PubMed: 22039301     


HMC-1.2 cells were cultured in the absence or presence of GSK3β inhibitor (CHIR 99021, 3–30 µM) and viability cell count was assessed by trypan blue dye exclusion after 24 h, 48 h or 72 h. All data are presented as the mean ± SEM of three independent experiments conducted in triplicate. p < 0.05*, p < 0.001** p < 0.0001*** vs vehicle treated control cells.

22039301
Immunofluorescence
SOX10 / EdU; 

PubMed: 28174705     


Incorporation of EdU (white arrowheads) into SOX10+ ENS (enteric nervous system) cells with and without CHIR-99021.

Oct3/4; 

PubMed: 24779365     


Fluorescence micrographs showing the protein expression of Brachyury/Oct3/4 after a three day differentiation of ES-D3 cells with BIO (0.5 μM), SB-216763 (5 μM), CHIR-99021 (5 μM), or CHIR-98014 (1 μM). Nuclei were counterstained with DAPI (blue). The merge is shown in yellow. Original magnification 400x. Scale bar = 50 μm.

28174705 24779365
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]

- 合并

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]

- 合并
  • 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]

- 合并
  • 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
储存条件 粉状
溶于溶剂
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 (mg) = 浓度 (mM) x 体积 (mL) 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID