Laduviglusib (CHIR-99021) HCl

目录号:S2924 别名: CT99021 HCl

仅限科研使用

Laduviglusib (CHIR-99021) 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。

Laduviglusib (CHIR-99021) HCl Chemical Structure

CAS: 1797989-42-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2780.99 现货
RMB 1373.92 现货
RMB 4650.09 现货
RMB 8330.15 现货
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客户使用Selleck生产的Laduviglusib (CHIR-99021) HCl发表文献469篇:

产品安全说明书

GSK-3抑制剂选择性比较

相关GSK-3产品

生物活性

产品描述 Laduviglusib (CHIR-99021) 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
NCI-H1581 Mny4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTlyMD6yN|Eh|ryP M1Xj[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H1155 NGn5e3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW5TWM2OD16MUiuNFU6KM7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
BC-3 NUi5OlgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[5fmlEPTB;OEC1MlIxOyEQvF2= NX7ncYo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
KARPAS-422 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\INoJCUUN3ME23PFkvOzF3IN88US=> NH;hRZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
DEL NGDkRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXTT5dKSzVyPUewNE45OzhizszN MoTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KM-H2 Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDmTWM2OD14OUmuNFU6KM7:TR?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
U-87-MG M{DaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTZ7ND61PFUh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 M{PHT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTZ7MD6xO|Ih|ryP NGjufXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
NCI-SNU-16 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvYdFFKSzVyPU[4NE41PjJizszN M4DlNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
TUR MonaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHSTWM2OD14N{GuN|IzKM7:TR?= MnrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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L-363 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrteHN2UUN3ME22OFgvODZ2IN88US=> MljlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
NCI-H226 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHuzRm1KSzVyPU[yPE4{PTNizszN M3fxVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HT MkjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TCVWlEPTB;NkKyMlc5PSEQvF2= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
KARPAS-45 MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT3WlNKSzVyPU[xPE4zOjFizszN MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
ML-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\VTWM2OD14ME[uOVc6KM7:TR?= NXXmeIRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
LP-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jx[2lEPTB;NkCzMlU5PyEQvF2= M2HNbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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K052 M4K1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPMS3A4UUN3ME21O|kvOjF|IN88US=> NUntUFZ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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RT-112 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPWV49{UUN3ME23MlE3PDV4IN88US=> NH[2XI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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LB2518-MEL NF;yeFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n0S2lEPTB;NT63NlYzPyEQvF2= M4[4blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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NCI-H2452 M2fFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O5cmlEPTB;NT60OVYzQCEQvF2= NILQUYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
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RCC10RGB NVPF[3RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTRwMkm0O|kh|ryP M2S1NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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MOLT-16 MoXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInlNmhKSzVyPUOuPFg2PTZizszN MnfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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HOP-62 NGXVOGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTNwM{[wOVQh|ryP NVjROo1FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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RPMI-7951 NFu0OlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJwN{CxPVMh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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NCI-H2122 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G1W2lEPTB;Mj6yO|Y5PCEQvF2= M2DjNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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MIA-PaCa-2 NFj3O21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XkVGlEPTB;MT63OVk4PyEQvF2= MnTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
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LOXIMVI NUjRU45WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwNUi4N|Ih|ryP NF;4NIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK|5USU6JRWK8M4E,
769-P M{\NdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjYdI9KSzVyPUCuOVg1QTlizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
GCT NWW2em9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLHTWM2OD1yLkOwOlczKM7:TR?= NXL3TVJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
SW982 NIHuXmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH0TWM2OD1yLkKxOFE3KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
ES-CCE MVzGeY5kfGmxbjDBd5NigQ>? NH;LTpQ2yqEQvF2= MUizJIQ> NVTReINYTE2VTx?= MX;TeJJwdmeueTDpcoR2[2W|IITo[UBi[3Srdnn0fUBw\iCZboSvZoV1[S2lYYTlcolvKHCjdHj3ZZk> NHTkNXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVM3PSd-MkS3O|k{PjV:L3G+
ES-D3 MlLUSpVv[3Srb36gRZN{[Xl? NE\K[W82yqEQvF2= Mn:zN{Bl NFW1b2FFVVOR M1T2eXN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
ES-CCE M4HYNmN6fG:2b4jpZ{BCe3OjeR?= M4n2XVExyqEQvF2= NIHQNmI{KGR? NV74V4R5TE2VTx?= M3m2fGlv\HWlZYOgcY9l\XKjdHWgZ5l1d3SxeHnjbZR6 NUTSS3ZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3O|k{PjVpPkK0O|c6OzZ3PD;hQi=>
ES-D3 M3[xPGN6fG:2b4jpZ{BCe3OjeR?= M2\aflExyqEQvF2= NY\UeVBWOyCm MX\EUXNQ NXfNS2E6UW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHlid3n0bEBKSzVyIH;mJFQvQSEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUO2OUc,OjR5N{mzOlU9N2F-
Neural progenitor cells MVTGeY5kfGmxbjDBd5NigQ>? NGL1V|Y{KM7:TR?= NIjze20yOCCm MV3EUXNQ MWXJcoR2[2W|IHflcoVz[XSrb36gc4YhdmW3cnHsJJBzd2enbnn0c5Ih[2WubIO= M2PZUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkO4NFM1Lz5{NE[zPFA{PDxxYU6=
A549 NGSxWHBCeG:ydH;zbZMhSXO|YYm= MUS1JOK2VQ>? NELUVpczPCCq NHfQNmtFVVOR M3;icWlv[3KnYYPld{Bk\WyuIHHwc5B1d3Orcx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4N{[4PEc,OjR|Nke2PFg9N2F-
H157 MVLBdI9xfG:|aYOgRZN{[Xl? Ml3POUDDvU1? M2PiPVI1KGh? MlvoSG1UVw>? MUjEc4V{KG6xdDDzbYdvcW[rY3HueIx6KGGoZnXjeEBieG:ydH;zbZM> M1zO[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
H460 MYTBdI9xfG:|aYOgRZN{[Xl? MlzzOUDDvU1? MUOyOEBp NXf4clVCTE2VTx?= MknGRZR1\W63YYTld{Bk\WyuIHHwc5B1d3Orcx?= NELQfnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2O|Y5QCd-MkSzOlc3QDh:L3G+
H157 M3HIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrEOUDDvU1? MoXFNlQhcA>? NFPiO3VFVVOR NIX0NnpRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> MmnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nke2PFgoRjJ2M{[3Olg5RC:jPh?=
H460 M2TFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfUOoM2KML3TR?= NYXk[ll7OjRiaB?= MUXEUXNQ NHPaVYxRem:vb4Tld{Bk\WyuIIDyc4xq\mW{YYTpc44> M1vyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[3Olg5Lz5{NEO2O|Y5QDxxYU6=
embryonic stem cells (ESC) NXnQcFNxTnWwY4Tpc44hSXO|YYm= MVqzJOK2VQ>? MkT4NVEh\A>? MlTlSG1UVw>? M3;iWnBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= M4\JeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OESzN|EzLz5{M{i0N|MyOjxxYU6=
DN3 M2TxdGZ2dmO2aX;uJGF{e2G7 NVHGbIJkOTBizszN MY[5OkBp MXLEUXNQ NWXzUlZ5UW6lcnXhd4V{KGOnbHyg[IV3\WyxcH3lcpQh[W6mIIDyc4xq\mW{YYTpc44> NXLwVWJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NlY6QDlpPkKzOVI3QTh7PD;hQi=>
platelets MkjtSpVv[3Srb36gRZN{[Xl? M3rlb|ExKM7:TR?= Mn\FNVUhdWmw M4f4fmROW09? NF7qV4ZKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? NIDHenM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPVg4Pyd-MkOyN|k5Pzd:L3G+
hiPSC-NPs MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP2N-KBkc7:TR?= M4DmSVczKGh? NUfWe|BtTE2VTx?= Mk\PTY5kemWjc3XzJINmdGxicILvcIln\XKjdHnvcuKh NEnKPY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[0NlY5Pyd-MkK2OFI3QDd:L3G+
INS-1E MoPQSpVv[3Srb36gRZN{[Xl? NVTmVlMzOi53IN88US=> MnywNlQhcA>? MV7EUXNQ MlrnTY5lfWOnczDhJJJm\HWldHnvckBw\iCQUEGgc5ZmemW6cILld5Nqd25? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR{N{ewOEc,OjJ2Mke3NFQ9N2F-
PANC1 NHPLZ|ZCeG:ydH;zbZMhSXO|YYm= MoSxxsA2KM7:TR?= MmfSO|IhcA>? MVnEUXNQ NXXNdnJ5XHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn NYOwcpNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFEyQDZpPkKyNlAyOTh4PD;hQi=>
Endothelial cell(EC) MX\GeY5kfGmxbjDBd5NigQ>? NXfCTog{OyEQvF2= M2HUfGROW09? MWDQdo9ud3SnczDlcoRwfGinbHnhcEBk\WyuIDjFR{kh\GmoZnXy[Y51cWG2aX;u NIXIU4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC1NlAxPid-MkKwOVIxODZ:L3G+
HMC1.2 NUT3c|RzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXBWpY{OCEQvF2= M3PScFczKGh? MVnEUXNQ MVLS[YR2[2W|IHPlcIwhe3W{dnn2ZYw> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB|OUOwNUc,OjJyM{mzNFE9N2F-
Sca-1+ HPC NVnDVZZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:yJO69VQ>? M{T2V|Yh\A>? MXXEUXNQ Mlr0V5lv\XKpaYP0bYNidGy7IIDyc41wfGW|IGPjZU0yM8LiSGDDJJBzd2yrZnXyZZRqd25iYX7kJINwdG:weTDmc5Ju[XSrb36geI9o\XSqZYKge4l1cCCHR1[= NX7XZopURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2NlQ{PDhpPkKxOlI1OzR6PD;hQi=>
Oct4/Sox2/Klf4-infected MEFs M1nJR2Z2dmO2aX;uJGF{e2G7 NHXIcmkyOCEQvF2= NHrpV5AzQCCm MYrEUXNQ NIPWUHBRem:vb4Tld{BOTU[|IILldJJw\3KjbX3pcochXHKjboPkeYNm\CCkeTDPZ5Q1NCCVb4iyMEBidmRiS3zmOC=> MmPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6M{mwOVUoRjF7OEO5NFU2RC:jPh?=
H4IIE NHrNe4dHfW6ldHnvckBCe3OjeR?= MX2xNEDPxE1? NWLO[WNxOjRiaB?= MkjNSG1UVw>? NIrhVFBT\We3bHH0[ZMh|rJvY3H0[Y5qdiCjY4Tpeol1gSCjbnSgWGlTTSClb370ZYlvcW6pIIDyc41wfGW{IHHjeIl3cXS7 Mn3jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV|NUCxPVUoRjF3M{WwNVk2RC:jPh?=
insulin receptor–expressing CHO-IR MkLLSpVv[3Srb36gRZN{[Xl? MoDoOVAxKG6P NFnKXY4{OCCvaX6= MVzEUXNQ MVnBZ5RqfmG2ZYOgS4x6[2:pZX6gV5lvfGijc3WgLGdUMQ>? NVHwOYtSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2NFY1QTdpPkGyOlA3PDl5PD;hQi=>
3T3-L1 NEi5W4pHfW6ldHnvckBCe3OjeR?= M2\ldFMh|ryP NXjhUFA5PCCq MXzEUXNQ NXT6SpFtUW6qaXLpeJMheHKnYXTpdI9kgXSnIHTp[oZmemWwdHnheIlwdg>? NGPLfVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkC1OVIxOCd-MUKwOVUzODB:L3G+
CHO-IR NG\WO|lHfW6ldHnvckBCe3OjeR?= MVSzNEBucW5? M2nOPGVEPTB;MD63O{DPxE1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTBzNkGyNUc,OjlyMU[xNlE9N2F-
HepG2 M{TtSmZ2dmO2aX;uJGF{e2G7 NULtNXZ2OyCq M2nXR2VEPTB;MT61JO69VQ>? NHT2VW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2NVAzOyd-MkKyOlExOjN:L3G+
Assay
Methods Test Index PMID
Western blot Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin CTNNB1 β-catenin 30709379 23993102 24165128
Growth inhibition assay Cell viability 22039301
Immunofluorescence SOX10 / EdU Oct3/4 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]

  • 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]

  • 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。

动物实验:

[1]

  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

技术支持

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操作手册

如果有其他问题,请给我们留言。

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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.