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。

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RMB 2780.99 现货
RMB 733.53 现货
RMB 1373.92 现货
RMB 4650.09 现货
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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 MVjGeY5kfGmxbjDBd5NigQ>? MXuzJO69VQ>? MoDKOEBp M3;rXWROW09? Mn3pTY5pcWKrdIOgdJJm[WSrcH;jfZRmKGSrZn\ldoVvfGmjdHnvci=> MX6xNlA2PTJyMB?=
insulin receptor–expressing CHO-IR NFPNNXpHfW6ldHnvckBCe3OjeR?= NGLNS4s2ODBibl2= MYKzNEBucW5? NYD2Z4VZTE2VTx?= MnHqRYN1cX[jdHXzJGdtgWOxZ3XuJHN6dnSqYYPlJEhIWyl? MYOxNlYxPjR7Nx?=
H4IIE NX7OVIZwTnWwY4Tpc44hSXO|YYm= NY\LblBUOTBizszN MXKyOEBp NXm1fHZnTE2VTx?= NFrpVndT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 NXLRe2JyOTV|NUCxPVU>
Oct4/Sox2/Klf4-infected MEFs M1HhPGZ2dmO2aX;uJGF{e2G7 M4PGcVExKM7:TR?= NGSwbpMzQCCm NX3KcFlVTE2VTx?= MUjQdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= NVL5[pFyOTl6M{mwOVU>
Sca-1+ HPC M1q2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPMbHhROiEQvF2= MYW2JIQ> MYHEUXNQ M2i5cHN6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG MYSyNVYzPDN2OB?=
HMC1.2 NX64ZWllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHJeIk{OzBizszN Mlz2O|IhcA>? NV36VmVYTE2VTx?= NFLTbopT\WS3Y3XzJINmdGxic4Xyeol3[Wx? MnjVNlIxOzl|MEG=
Endothelial cell(EC) Ml;WSpVv[3Srb36gRZN{[Xl? NV30SY4zOyEQvF2= MkPwSG1UVw>? MYrQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u NECwfHczOjB3MkCwOi=>
PANC1 NWLsbZJoSXCxcITvd4l{KEG|c3H5 M{nNZeKhPSEQvF2= MnPLO|IhcA>? NYjsc2d1TE2VTx?= NVjEZ2NjXHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn M16zTFIzOjBzMUi2
INS-1E NFW4dnNHfW6ldHnvckBCe3OjeR?= MXuyMlUh|ryP M3LvOlI1KGh? NHPxelRFVVOR NGLGN3dKdmS3Y3XzJIEhemWmdXP0bY9vKG:oIF7QNUBwfmW{ZYjwdoV{e2mxbh?= MkXNNlI1Ojd5MES=
hiPSC-NPs NVy2WFhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHlRXBYO+LCid88US=> NGGzNm84OiCq M2DobmROW09? NUn1ZXdwUW6lcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdsLi MUeyNlY1OjZ6Nx?=
platelets MnPwSpVv[3Srb36gRZN{[Xl? MnfnNVAh|ryP MkfFNVUhdWmw MmXzSG1UVw>? NHHXdZlKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? MlO2NlMzOzl6N{e=
DN3 MkPmSpVv[3Srb36gRZN{[Xl? M2nDUVExKM7:TR?= M{DjZlk3KGh? MkPTSG1UVw>? NELiOm1KdmO{ZXHz[ZMh[2WubDDk[ZZmdG:ybXXueEBidmRicILvcIln\XKjdHnvci=> MkTENlM2OjZ7OEm=
embryonic stem cells (ESC) MoTNSpVv[3Srb36gRZN{[Xl? MkG1N{DDvU1? MlXzNVEh\A>? MXzEUXNQ MnXHVJJwdW:2ZYOgd4Vt\i2{ZX7le4FtKG:oIH7hx893\S22eYDlJI1wfXOnIHXtZpJ6d26rYzDzeIVuKGOnbHzzJEhGW0Nr MXOyN|g1OzNzMh?=
H460 MnrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS1JOK2VQ>? NX\jdoN2OjRiaB?= NHf2N4RFVVOR MX;Qdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= NG\Yb5UzPDN4N{[4PC=>
H157 M4D5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\HNVUhyrWP MXmyOEBp Mk\ZSG1UVw>? NF\4ZYdRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> NFT3[FAzPDN4N{[4PC=>
H460 NITKeG5CeG:ydH;zbZMhSXO|YYm= NGW0bI82KML3TR?= MlHkNlQhcA>? MlLKSG1UVw>? NUfybHNZSXS2ZX71ZZRmeyClZXzsJIFxd3C2b4Ppdy=> NE\XWXMzPDN4N{[4PC=>
H157 MWjBdI9xfG:|aYOgRZN{[Xl? MV21JOK2VQ>? M13BS|I1KGh? M1TYTGROW09? NFvyPIlFd2W|IH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCjcH;weI9{cXN? Mn3SNlQ{Pjd4OEi=
A549 MVzBdI9xfG:|aYOgRZN{[Xl? NF3pR3g2KML3TR?= NV32c5M4OjRiaB?= NELjbGFFVVOR NEXmS|FKdmO{ZXHz[ZMh[2WubDDhdI9xfG:|aYO= NEPZNnYzPDN4N{[4PC=>
Neural progenitor cells NVq1SmlvTnWwY4Tpc44hSXO|YYm= MVqzJO69VQ>? M1LnO|ExKGR? MnzNSG1UVw>? M{jZUmlv\HWlZYOg[4Vv\XKjdHnvckBw\iCwZYXyZYwheHKxZ3XubZRweiClZXzsdy=> MmT5NlQ3OzhyM{S=
ES-D3 M1Pz[GN6fG:2b4jpZ{BCe3OjeR?= MnzHNVDDqM7:TR?= NIjJV4Q{KGR? NUnUcHdTTE2VTx?= MXjJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fUB4cXSqIFnDOVAhd2ZiND65JO69VQ>? M2qyZVI1Pzd7M{[1
ES-CCE NUHibFVCS3m2b4TvfIlkKEG|c3H5 M{SzO|ExyqEQvF2= MYezJIQ> MVvEUXNQ NUTBemdKUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHl? NIPVcWEzPDd5OUO2OS=>
ES-D3 NVLYNmQ2TnWwY4Tpc44hSXO|YYm= MUi1xsDPxE1? M323PVMh\A>? MorjSG1UVw>? M{jxN3N1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? MYmyOFc4QTN4NR?=
ES-CCE MVHGeY5kfGmxbjDBd5NigQ>? NYizSHFTPcLizszN MlnHN{Bl M1j2OGROW09? M{XMc3N1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? MkjKNlQ4Pzl|NkW=
SW982 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMkG0NVYh|ryP Mn3vV2FPT0WU
GCT MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPSTWM2OD1yLkOwOlczKM7:TR?= NX3KNlI5W0GQR1XS
769-P NXTLTnU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e3TmlEPTB;MD61PFQ6QSEQvF2= MVvTRW5ITVJ?
LOXIMVI NXvzbnUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwNUi4N|Ih|ryP NWXuXJlYW0GQR1XS
D-336MG M3TZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTzcmgzUUN3ME2wMlg1PjJizszN NVnobG9tW0GQR1XS
S-117 Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD6TWM2OD1yLkmyNVMyKM7:TR?= MmPPV2FPT0WU
D-247MG MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwOUS4OVIh|ryP NHziWm5USU6JRWK=
TYK-nu M{WxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\XR2lEPTB;MT6wO|kyOiEQvF2= MojtV2FPT0WU
A498 M{PqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwM{C0Olkh|ryP Mle3V2FPT0WU
BCPAP NX7vZWI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DwVWlEPTB;MT62Olg6QCEQvF2= M4fSXnNCVkeHUh?=
KYSE-180 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFwN{K3PFgh|ryP NITGNnBUSU6JRWK=
MIA-PaCa-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLEd2RpUUN3ME2xMlc2QTd5IN88US=> MlzaV2FPT0WU
HCC1395 M1P3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fhR2lEPTB;MT63PFI4OyEQvF2= MXrTRW5ITVJ?
RS4-11 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfWOYN4UUN3ME2xMlk2PDF3IN88US=> MnLUV2FPT0WU
NCI-H2122 M1PsOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzKcVFKUUN3ME2yMlI4Pjh2IN88US=> MVzTRW5ITVJ?
SNU-423 NVThfYZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXUTWM2OD1{LkS5O|g4KM7:TR?= Mny3V2FPT0WU
SK-LMS-1 NVXENpJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfZepNKSzVyPUKuOlQyOjhizszN MlrxV2FPT0WU
RPMI-7951 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jrZ2lEPTB;Mj63NFE6OyEQvF2= MYjTRW5ITVJ?
COLO-829 M1jOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\BfWlEPTB;Mj63OlU1KM7:TR?= Mn63V2FPT0WU
SCC-9 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfCTWM2OD1{Lkm1OFg2KM7:TR?= NUDTTmtIW0GQR1XS
A704 NXnoSHpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m2O2lEPTB;Mz6wPFEzKM7:TR?= NHPiSJJUSU6JRWK=
HOP-62 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXGTWM2OD1|LkO2NFU1KM7:TR?= NH22NFZUSU6JRWK=
HCC1569 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfNT5VTUUN3ME2zMlQ5OzB3IN88US=> NV;DTHl3W0GQR1XS
A172 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK0WpVJUUN3ME2zMlc2PDl6IN88US=> M{XUXnNCVkeHUh?=
MOLT-16 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDhTWM2OD1|Lki4OVU3KM7:TR?= NHixc29USU6JRWK=
TE-15 M1LCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTNwOUWzOFMh|ryP NES3SmlUSU6JRWK=
OE19 NYDXNoh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwOU[0OVEh|ryP NIGyWIFUSU6JRWK=
MHH-ES-1 NHTTc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTRwMES1OFUh|ryP M3fwNnNCVkeHUh?=
NKM-1 M{PWR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLPWJFwUUN3ME20MlE{QTdzIN88US=> NWPzV3hCW0GQR1XS
RCC10RGB NV3QTop5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrI[2FKSzVyPUSuNlk1PzlizszN MUnTRW5ITVJ?
BxPC-3 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnUfmdKSzVyPUSuO|A{QTFizszN MmrsV2FPT0WU
ALL-PO MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4r3WGlEPTB;ND64N|g2QCEQvF2= NXrYSI0zW0GQR1XS
SK-OV-3 M2DTfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH5V3JKSzVyPUSuPVk{PCEQvF2= Ml\lV2FPT0WU
SW1710 NGPjPZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF70NGhKSzVyPUWuOFI1PTZizszN NE\mWINUSU6JRWK=
NCI-H2452 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTVwNEW2Nlgh|ryP MkPiV2FPT0WU
D-392MG NWPscYRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnWbmNSUUN3ME21MlQ6OTR3IN88US=> MkXIV2FPT0WU
LB2518-MEL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz3XYJKSzVyPUWuO|I3OjdizszN MYLTRW5ITVJ?
BL-41 M4DifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OySmlEPTB;NT64NVI3PiEQvF2= NEn3PVRUSU6JRWK=
WM-115 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i3ZmlEPTB;NT64NVUxQSEQvF2= NV;zVW1FW0GQR1XS
SK-MEL-2 NGDNflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDrTWM2OD14LkO4N|Q1KM7:TR?= Mm\wV2FPT0WU
CGTH-W-1 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTZwNEG3JO69VQ>? M2jQSHNCVkeHUh?=
BB65-RCC NEOzRYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHBcYZ3UUN3ME22MlU{OTl3IN88US=> MlnGV2FPT0WU
CAL-85-1 MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDWZmVKSzVyPU[uOlA6OzZizszN NIjTOnBUSU6JRWK=
RT-112 NGW4NpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X4emlEPTB;Nz6xOlQ2PiEQvF2= M1TZcHNCVkeHUh?=
MC116 M2rVfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\BXmlEPTB;Nz6yPFY6OSEQvF2= NYDhcnF7W0GQR1XS
G-361 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz2RZhKSzVyPUeuOFY2PjFizszN Mk\4V2FPT0WU
SW1417 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DNeWlEPTB;Nz62OFU5PCEQvF2= MYnTRW5ITVJ?
MV-4-11 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRThwNUSzNFQh|ryP NIXVeIpUSU6JRWK=
CAL-72 MkL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRThwN{[xNVMh|ryP M13NfnNCVkeHUh?=
MKN28 NYPKWFJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnaTWM2OD16Lki4OVE3KM7:TR?= M4nNTHNCVkeHUh?=
MEG-01 M{KxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\oUGlEPTB;OD65PVA1OyEQvF2= NWLaWXdNW0GQR1XS
ACHN NFzLOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr5TWM2OD17LkOwOVQ3KM7:TR?= NW\uUoVKW0GQR1XS
NCI-H1755 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlT2TWM2OD17LkO5PVg3KM7:TR?= NEnWfFdUSU6JRWK=
NCI-H64 NVPXUZNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTlwNEKyOVUh|ryP NInYTFVUSU6JRWK=
COLO-205 M2S5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfodYpKSzVyPUmuOFM5OjFizszN MkPNV2FPT0WU
CTV-1 NFPOWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIr2[INKSzVyPUmuOFM5QTRizszN MlKyV2FPT0WU
U-2-OS MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPuTWM2OD17LkS1NFA3KM7:TR?= M2\2PHNCVkeHUh?=
LB996-RCC M1Gzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jmWGlEPTB;OT61NlM6PyEQvF2= MkPnV2FPT0WU
SK-N-DZ MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3TTWM2OD17Lk[1O|QzKM7:TR?= M2\mTHNCVkeHUh?=
EFM-19 M2fZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vxcWlEPTB;OT63OVU3PiEQvF2= MlzXV2FPT0WU
DBTRG-05MG Ml3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\y[3VOUUN3ME25Mlc4PzdizszN MWDTRW5ITVJ?
U-118-MG MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfBTWM2OD17Lkm0OFQ1KM7:TR?= MkDVV2FPT0WU
LB1047-RCC MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfDTWM2OD17Lkm5O|k5KM7:TR?= NH3Kc4NUSU6JRWK=
NCI-H28 M4SwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnzZZFKSzVyPUGwMlQ1OTNizszN MV3TRW5ITVJ?
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OVCAR-5 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\RTWM2OD1zNkiuN|A6KM7:TR?= NVKzfo5KW0GQR1XS
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CP66-MEL MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF4OD60NVUh|ryP MVTTRW5ITVJ?
KYSE-150 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvZN4JKSzVyPUG2PU43OzZizszN MoPVV2FPT0WU
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SW620 NUPSO2FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTJdXlXUUN3ME2xO|EvPTN3IN88US=> M2\6ZXNCVkeHUh?=
HuO-3N1 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF5Mj6yO|Mh|ryP MnXLV2FPT0WU
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YT NYPFZotzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWe4cVlGUUN3ME2xO|YvOzl7IN88US=> MW\TRW5ITVJ?
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LB2241-RCC NGfVSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTF6NT6xOFUh|ryP NGPzTmxUSU6JRWK=
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MFM-223 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfYdnJHUUN3ME2yNFEvPTh5IN88US=> M4nCcXNCVkeHUh?=
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LAMA-84 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHzd|N6UUN3ME2yNFIvODd|IN88US=> MlLWV2FPT0WU
LS-1034 NWGw[plrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vwZmlEPTB;MkCyMlU2OyEQvF2= NVPjRnNWW0GQR1XS
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KYSE-70 NUTweph3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5N4RPUUN3ME2yNFMvQDd7IN88US=> MUPTRW5ITVJ?
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NCI-H1651 NHjXfodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fWZWlEPTB;MkC2Mlc{KM7:TR?= M1jMXnNCVkeHUh?=
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NUGC-3 NHHTVm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkThTWM2OD1{MEmuOlc5KM7:TR?= M2HwXnNCVkeHUh?=
DJM-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\NT3c1UUN3ME2yNFkvQDl5IN88US=> Mm\FV2FPT0WU
MHH-PREB-1 MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\vTWM2OD1{MUCuN|gyKM7:TR?= MWPTRW5ITVJ?
EW-18 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPRPW5ZUUN3ME2yNVAvPzZ|IN88US=> MXPTRW5ITVJ?
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NCI-H2081 NEC2WGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PPc2lEPTB;NUK1MlUyOyEQvF2= M{HqfXNCVkeHUh?=
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HSC-4 NH\CU2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTV|OT6yPVMh|ryP MVLTRW5ITVJ?
RL NX7jeHByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7zbIhKSzVyPUW0Nk41PDJizszN MX\TRW5ITVJ?
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NCI-H889 M2fITGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\KTWM2OD13NEeuNlMh|ryP M{HQR3NCVkeHUh?=
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UACC-812 MoPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjHbm9HUUN3ME21OVkvOzlzIN88US=> NVH0bGVFW0GQR1XS
CAL-148 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILZfplKSzVyPUW2OU4xQDlizszN NEfiOXBUSU6JRWK=
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LP-1 NIH5[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIT3VZhKSzVyPU[wN{42QDdizszN MnXsV2FPT0WU
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TUR M3PIe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TtSWlEPTB;NkexMlMzOiEQvF2= NXqxXWJ7W0GQR1XS
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KARPAS-422 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1m2eWlEPTB;N{i5MlMyPSEQvF2= M1zkR3NCVkeHUh?=
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NCI-H1155 NV7OSXRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2P5WGlEPTB;OEG4MlA2QSEQvF2= MVXTRW5ITVJ?
NCI-H1581 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHkS3FKSzVyPUmwNE4zOzFizszN NXr5W5ZtW0GQR1XS

... 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]
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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：

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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：

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  • 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