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。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2780.99	现货
5mg	RMB 1373.92	现货
25mg	RMB 4650.09	现货
100mg	RMB 8330.15	现货
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客户使用Selleck生产的CHIR-99021 (CT99021) HCl发表文献409篇：

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Bachelor of Science, 2012, East China Normal University

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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

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	Activity Description	PMID
NCI-H1581	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mn3BTWM2OD17MECuNlMyKM7:TR?=	M4ThVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-H1155	MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIjYeo1KSzVyPUixPE4xPTlizszN	NX;yeoNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
BC-3	M4j1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{T3UGlEPTB;OEC1MlIxOyEQvF2=	NGTIRVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
KARPAS-422	M{\vXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkPpTWM2OD15OEmuN\|E2KM7:TR?=	MoPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
DEL	MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV7JR\|UxRTdyMD64N\|gh\|ryP	MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KM-H2	MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIHiU2lKSzVyPU[5PU4xPTlizszN	M{jRXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
U-87-MG	NXXlSYZmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2LBfGlEPTB;Nkm0MlU5PSEQvF2=	M1rpWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
NCI-SNU-1	M2\qZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlL1TWM2OD14OUCuNVczKM7:TR?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
NCI-SNU-16	MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIrpWGdKSzVyPU[4NE41PjJizszN	M4rJVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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NOS-1	NHP0VXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGrsbYVKSzVyPUGzOE44PjVizszN	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
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CP50-MEL-B	NIL2OJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2P1eWlEPTB;MUO0MlIh\|ryP	M4jDfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
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CTB-1	MoHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3zZcWlEPTB;MUOyMlg6PyEQvF2=	NGPTRZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
HT-1080	M4HrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkDITWM2OD1zM{KuNlA1KM7:TR?=	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
MFH-ino	NWi0XXdOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4fsUWlEPTB;MUOxMlEyPCEQvF2=	NHrRPGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
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HEC-1	NFHEZZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmPqTWM2OD1zMkmuNVk5KM7:TR?=	NFjwZ\|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
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UMC-11	M1LKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVrYeIVsUUN3ME2xNlYvODN6IN88US=>	NHHzW4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
NCI-H2087	M2OzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWTkWHdmUUN3ME2xNlQvOjh\|IN88US=>	M4ftOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
SW1463	NFHYe41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVPJR\|UxRTF{ND6wO\|ch\|ryP	NWjFZ2lrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
OPM-2	Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH7sR49KSzVyPUGyN{4yPzZizszN	M{ezTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
HT-29	M1rwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUSybmZ7UUN3ME2xNlIvPzd6IN88US=>	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
HAL-01	NEPWTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MWrJR\|UxRTF{Mj60PVkh\|ryP	MmLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KYSE-140	NXXxS4FuT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVnhdWFmUUN3ME2xNlIvOTRzIN88US=>	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
HuP-T4	Mm\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NInzeY9KSzVyPUGyNU42PSEQvF2=	NIn6XZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1OTJzNEKvK\|5USU6JRWK8M4E,
NCI-N87	MmC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1W4d2lEPTB;MUKxMlA1PCEQvF2=	M3LBUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQyOjF2Mj:nQnNCVkeHUkyvZV4>
OVCAR-3	MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWrJR\|UxRTFzOT65NVUh\|ryP	MkX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
KNS-81-FD	NV\CXGV3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWfoVHBzUUN3ME2xNVkvPDF5IN88US=>	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0NVIyPDJxJ{7TRW5ITVJ:L3G+
SUP-T1	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml[2TWM2OD1zMUiuPVU3KM7:TR?=	MkXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFEzOTR{Lze+V2FPT0WUPD;hQi=>
SKG-IIIa	NHu0V\|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnvZTWM2OD1zMUiuNVE3KM7:TR?=	NXTRUnRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
RKO	M2L4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MW\JR\|UxRTFzNz64PVgh\|ryP	NUW5VIM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
ATN-1	NYLkU\|V3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mlf5TWM2OD1zMUeuPFI5KM7:TR?=	NYLZO5pXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDF{MUSyM{c,W0GQR1XSQE9iRg>?
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SW1573

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