CHIR-99021 (CT99021) HCl

For research use only. Not for use in humans.

目录号：S2924

CHIR-99021 (CT99021) HCl Chemical Structure

CAS No. 1797989-42-4

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。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。

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客户使用Selleck生产的CHIR-99021 (CT99021) HCl发表文献250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。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。
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 NELQO2VHfW6ldHnvckBCe3OjeR?= NF7NOZM{KM7:TR?= MkD1OEBp MWjEUXNQ NUnPSG9EUW6qaXLpeJMheHKnYXTpdI9kgXSnIHTp[oZmemWwdHnheIlwdg>? MXmxNlA2PTJyMB?=
insulin receptor–expressing CHO-IR MXnGeY5kfGmxbjDBd5NigQ>? MYW1NFAhdk1? NFrFflU{OCCvaX6= NIPz[5ZFVVOR NXyzN5VGSWO2aY\heIV{KEeueXPv[4VvKFO7boToZZNmKCiJUzm= M3nP[lEzPjB4NEm3
H4IIE NXHoOFRJTnWwY4Tpc44hSXO|YYm= M3XITlExKM7:TR?= M1;iNlI1KGh? NVLlVFBHTE2VTx?= NE\wV|lT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 M4[2WVE2OzVyMUm1
Oct4/Sox2/Klf4-infected MEFs M1;6fWZ2dmO2aX;uJGF{e2G7 MUKxNEDPxE1? MoG5Nlgh\A>? NWm4fHFRTE2VTx?= MWfQdo9ud3SnczDNSWZ{KHKncILv[5JidW2rbnegWJJidnOmdXPl[EBjgSCRY4S0MEBUd3h{LDDhcoQhU2yoNB?= NUPpeZVoOTl6M{mwOVU>
Sca-1+ HPC NY[0UZZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUCyJO69VQ>? MVK2JIQ> MVrEUXNQ NIDDc2tUgW6ncnfpd5Rq[2GubImgdJJwdW:2ZYOgV4NiNTFtwrDIVGMheHKxbHnm[ZJifGmxbjDhcoQh[2:ub375JIZwem2jdHnvckB1d2endHjldkB4cXSqIFXHSi=> NGHTeIQzOTZ{NEO0PC=>
HMC1.2 M2fCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\sN|Ah|ryP NXnzPHJOPzJiaB?= M1PKNmROW09? MYPS[YR2[2W|IHPlcIwhe3W{dnn2ZYw> MlH5NlIxOzl|MEG=
Endothelial cell(EC) M2PS[WZ2dmO2aX;uJGF{e2G7 NU[w[pFLOyEQvF2= M2nnNWROW09? NV3kTYxZWHKxbX;0[ZMh\W6mb4To[Yxq[WxiY3XscEApTUNrIHTp[oZmemWwdHnheIlwdg>? Mk[0NlIxPTJyME[=
PANC1 NEK1PYdCeG:ydH;zbZMhSXO|YYm= NET1SmbDqDVizszN MVO3NkBp MVzEUXNQ NV32fml{XHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn NX3wXIlROjJ{MEGxPFY>
INS-1E MoX2SpVv[3Srb36gRZN{[Xl? NGXpW3QzNjVizszN MXOyOEBp MnnQSG1UVw>? MYfJcoR2[2W|IHGgdoVlfWO2aX;uJI9nKE6SMTDveoVz\XiycnXzd4lwdg>? MX2yNlQzPzdyNB?=
hiPSC-NPs MljlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPQN-KBkc7:TR?= M2D1W|czKGh? NGjFdWJFVVOR M33CWWlv[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc47DqA>? NGfOR4IzOjZ2Mk[4Oy=>
platelets NW\seGdITnWwY4Tpc44hSXO|YYm= NIXXVpMyOCEQvF2= MUOxOUBucW5? MofSSG1UVw>? MXvJcoNz\WG|ZYOgeIhzd22kaX6tcYVlcWG2ZXSgdIxifGWuZYSgZYdoemWpYYTpc44h[W6mIFHUVEB{\WO{ZYTpc44> M3znSFI{OjN7OEe3
DN3 MkewSpVv[3Srb36gRZN{[Xl? M{DIXVExKM7:TR?= NX\pcnVpQTZiaB?= NFHoVZZFVVOR Mn\oTY5kemWjc3XzJINmdGxiZHX2[YxweG2nboSgZY5lKHC{b3zp[oVz[XSrb36= M1nWOlI{PTJ4OUi5
embryonic stem cells (ESC) NX\zfGpqTnWwY4Tpc44hSXO|YYm= Mln0N{DDvU1? MVuxNUBl M{\E[mROW09? Mn2yVJJwdW:2ZYOgd4Vt\i2{ZX7le4FtKG:oIH7hx893\S22eYDlJI1wfXOnIHXtZpJ6d26rYzDzeIVuKGOnbHzzJEhGW0Nr NY\qeoJCOjN6NEOzNVI>
H460 NVjjSWIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXG1JOK2VQ>? MWOyOEBp MWnEUXNQ MXLQdo9ud3SnczDj[YxtKHC{b3zp[oVz[XSrb36= MYGyOFM3PzZ6OB?=
H157 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37rWlUhyrWP NH;nZZAzPCCq MWrEUXNQ MmTlVJJwdW:2ZYOgZ4VtdCCycn;sbYZmemG2aX;u MUWyOFM3PzZ6OB?=
H460 NFLIWJZCeG:ydH;zbZMhSXO|YYm= MXy1JOK2VQ>? MV6yOEBp NFr0boFFVVOR M1PEW2F1fGWwdXH0[ZMh[2WubDDhdI9xfG:|aYO= MoPMNlQ{Pjd4OEi=
H157 MX7BdI9xfG:|aYOgRZN{[Xl? MnLsOUDDvU1? Mn3rNlQhcA>? MkKwSG1UVw>? MX3Ec4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> NUTnPJBjOjR|Nke2PFg>
A549 NEC4N|VCeG:ydH;zbZMhSXO|YYm= MWS1JOK2VQ>? NGjLc3EzPCCq M1;nb2ROW09? MWnJcoNz\WG|ZYOgZ4VtdCCjcH;weI9{cXN? MYSyOFM3PzZ6OB?=
Neural progenitor cells M1r5bGZ2dmO2aX;uJGF{e2G7 NXrOOYxGOyEQvF2= MnLJNVAh\A>? NUjjSIdSTE2VTx?= NUGyOnF3UW6mdXPld{Bo\W6ncnH0bY9vKG:oIH7leZJidCCycn;n[Y5qfG:{IHPlcIx{ MmqwNlQ3OzhyM{S=
ES-D3 NHHxeIVEgXSxdH;4bYMhSXO|YYm= M2TZXlExyqEQvF2= NIj1eJc{KGR? MXfEUXNQ M{jVXGlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6KHerdHigTWM2OCCxZjC0Mlkh|ryP NIT4W5MzPDd5OUO2OS=>
ES-CCE NILPT5dEgXSxdH;4bYMhSXO|YYm= MkO3NVDDqM7:TR?= NX3hWmQ1OyCm Mn\XSG1UVw>? NVfDfXptUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHl? MUiyOFc4QTN4NR?=
ES-D3 MWHGeY5kfGmxbjDBd5NigQ>? NGXj[YY2yqEQvF2= Mn\TN{Bl MYLEUXNQ M1vsNnN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? Ml7pNlQ4Pzl|NkW=
ES-CCE NWfTUFJUTnWwY4Tpc44hSXO|YYm= MoTrOeKh|ryP Ml3CN{Bl MWLEUXNQ NHT2V21UfHKxbnfsfUBqdmS3Y3XzJJRp\SCjY4Tpeol1gSCxZjDXcpQw[mW2YT3jZZRmdmmwIIDheIh4[Xl? MnPJNlQ4Pzl|NkW=
SW982 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfKR21KSzVyPUCuNlE1OTZizszN Mon5V2FPT0WU
GCT MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ftRmlEPTB;MD6zNFY4OiEQvF2= NYrtZZI1W0GQR1XS
769-P NF6zXWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\JSGlEPTB;MD61PFQ6QSEQvF2= MUDTRW5ITVJ?
LOXIMVI MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj2Z49KSzVyPUCuOVg5OzJizszN Mn3IV2FPT0WU
D-336MG MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjtV2tlUUN3ME2wMlg1PjJizszN NXP0dlFsW0GQR1XS
S-117 NY\kWo55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvaTWM2OD1yLkmyNVMyKM7:TR?= NVq2WVVOW0GQR1XS
D-247MG MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PON2lEPTB;MD65OFg2OiEQvF2= MkexV2FPT0WU
TYK-nu MmrSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnIOYZKSzVyPUGuNFc6OTJizszN M4\rO3NCVkeHUh?=
A498 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG0TWM2OD1zLkOwOFY6KM7:TR?= M2nRcnNCVkeHUh?=
BCPAP M2qxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlKzTWM2OD1zLk[2PFk5KM7:TR?= Ml33V2FPT0WU
KYSE-180 NVvVbFh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LHU2lEPTB;MT63Nlc5QCEQvF2= M4ruV3NCVkeHUh?=
MIA-PaCa-2 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLUfJhkUUN3ME2xMlc2QTd5IN88US=> MmW3V2FPT0WU
HCC1395 Ml3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HWdWlEPTB;MT63PFI4OyEQvF2= MXzTRW5ITVJ?
RS4-11 MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFwOUW0NVUh|ryP NWnXPVk3W0GQR1XS
NCI-H2122 MoLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfnZY9lUUN3ME2yMlI4Pjh2IN88US=> M1fLSXNCVkeHUh?=
SNU-423 NHrtO3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXsT5JFUUN3ME2yMlQ6Pzh5IN88US=> NH7ON4JUSU6JRWK=
SK-LMS-1 M2OyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;NcHk{UUN3ME2yMlY1OTJ6IN88US=> NYTSdph6W0GQR1XS
RPMI-7951 NIexdXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLETWM2OD1{LkewNVk{KM7:TR?= M3m3SHNCVkeHUh?=
COLO-829 M1\mfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHviU3hKSzVyPUKuO|Y2PCEQvF2= NELYVGxUSU6JRWK=
SCC-9 NYjaZocxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJwOUW0PFUh|ryP M3LCNHNCVkeHUh?=
A704 M3r4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXyNoZKSzVyPUOuNFgyOiEQvF2= NWjFV3FFW0GQR1XS
HOP-62 NXvOe21TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2W5fmlEPTB;Mz6zOlA2PCEQvF2= NH3weHhUSU6JRWK=
HCC1569 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTNwNEizNFUh|ryP NFfo[HdUSU6JRWK=
A172 M13yS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTNwN{W0PVgh|ryP MWDTRW5ITVJ?
MOLT-16 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNwOEi1OVYh|ryP Mk\jV2FPT0WU
TE-15 NXvjTVltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTNwOUWzOFMh|ryP MWTTRW5ITVJ?
OE19 NV;3clFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTNwOU[0OVEh|ryP M2nYW3NCVkeHUh?=
MHH-ES-1 NEDmW4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK3NoFKSzVyPUSuNFQ2PDVizszN MWPTRW5ITVJ?
NKM-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PwTWlEPTB;ND6xN|k4OSEQvF2= NUTFSYk6W0GQR1XS
RCC10RGB MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rCUWlEPTB;ND6yPVQ4QSEQvF2= NGDWS5JUSU6JRWK=
BxPC-3 NXTHO4tzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTRwN{CzPVEh|ryP NU\ob41FW0GQR1XS
ALL-PO MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTRwOEO4OVgh|ryP MYnTRW5ITVJ?
SK-OV-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCzUoZNUUN3ME20Mlk6OzRizszN NHO0WHZUSU6JRWK=
SW1710 NGXucXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTVwNEK0OVYh|ryP NW\nWIszW0GQR1XS
NCI-H2452 NUHMSW5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDtbnY3UUN3ME21MlQ2PjJ6IN88US=> MV;TRW5ITVJ?
D-392MG NXKycpR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTVwNEmxOFUh|ryP M2SyO3NCVkeHUh?=
LB2518-MEL NVT5[XcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULUT29nUUN3ME21MlczPjJ5IN88US=> MlHuV2FPT0WU
BL-41 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTVwOEGyOlYh|ryP Mn7UV2FPT0WU
WM-115 NEfJ[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTVwOEG1NFkh|ryP NXLGdmE{W0GQR1XS
SK-MEL-2 M2TKeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LXdmlEPTB;Nj6zPFM1PCEQvF2= MVTTRW5ITVJ?
CGTH-W-1 MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHey[nJKSzVyPU[uOFE4KM7:TR?= MX3TRW5ITVJ?
BB65-RCC M1T1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHDOGNKSzVyPU[uOVMyQTVizszN M1TRUHNCVkeHUh?=
CAL-85-1 NVrFTVlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7YdWJKSzVyPU[uOlA6OzZizszN NE\l[FFUSU6JRWK=
RT-112 NWC1XplIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTdwMU[0OVYh|ryP MknSV2FPT0WU
MC116 NWjLTXFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzvbnFOUUN3ME23MlI5PjlzIN88US=> MkHiV2FPT0WU
G-361 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jBeWlEPTB;Nz60OlU3OSEQvF2= MnntV2FPT0WU
SW1417 MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXmTWM2OD15Lk[0OVg1KM7:TR?= NETNXmdUSU6JRWK=
MV-4-11 NUj2fmRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mor1TWM2OD16LkW0N|A1KM7:TR?= NXvnPZBjW0GQR1XS
CAL-72 NWjFVm5IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL3TWM2OD16Lke2NVE{KM7:TR?= NH;mfIJUSU6JRWK=
MKN28 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3MTWM2OD16Lki4OVE3KM7:TR?= NWi3PY8zW0GQR1XS
MEG-01 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRThwOUmwOFMh|ryP NY\nUIZCW0GQR1XS
ACHN NW\EdJN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrwT41KSzVyPUmuN|A2PDZizszN NYmwfHI5W0GQR1XS
NCI-H1755 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfzR2JKSzVyPUmuN|k6QDZizszN NH[5XpFUSU6JRWK=
NCI-H64 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL4[GVKSzVyPUmuOFIzPTVizszN NVr5fmV4W0GQR1XS
COLO-205 M2L3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XaSGlEPTB;OT60N|gzOSEQvF2= NFixNG1USU6JRWK=
CTV-1 NFrVcZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTlwNEO4PVQh|ryP NFj5ZndUSU6JRWK=
U-2-OS M2LTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfQe4lKSzVyPUmuOFUxODZizszN Mn;MV2FPT0WU
LB996-RCC MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXxTWM2OD17LkWyN|k4KM7:TR?= Ml\4V2FPT0WU
SK-N-DZ NFS0OVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXXWmRKUUN3ME25MlY2PzR{IN88US=> MYPTRW5ITVJ?
EFM-19 NYDUeVh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDYTWM2OD17Lke1OVY3KM7:TR?= Mn;GV2FPT0WU
DBTRG-05MG NE\CblBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPvTWM2OD17Lke3O|ch|ryP NIjZdGlUSU6JRWK=
U-118-MG NHHRRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16w[mlEPTB;OT65OFQ1PCEQvF2= NVHycmU2W0GQR1XS
LB1047-RCC NVW0VIZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfWOItKSzVyPUmuPVk4QThizszN NITpdGVUSU6JRWK=
NCI-H28 NFP1cYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HjZmlEPTB;MUCuOFQyOyEQvF2= MkTzV2FPT0WU
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Daudi MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHoWo9{UUN3ME2xO{43OTR7IN88US=> MmjVV2FPT0WU
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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
  • 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

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

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.

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。CHIR-99021 可作为Wnt/β-catenin的激活剂并诱导自噬。

  • 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 (NP 01139) 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。GSK-3β的抑制可触发自噬。

  • 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。SB216763 可激活自噬。

  • Tideglusib

    Tideglusib (NP031112, NP-12)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 (CT98014)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 (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime)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，对 Tyk2 的IC50值为30 nM。BIO 可在人类黑色素瘤细胞中诱导凋亡。

    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 (GSK-3β Inhibitor VIII)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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