|3-(2,4-二氯苯基)-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮|CsnPharm

CAS No.: 280744-09-4

3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione Catalog No. CSN12268

Synonyms: SB-216763

SB-216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 9 nM) and competes with ATP.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GSK-3

Ki:9nM
描述GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3 and subunit, which plays a key role in many different biological processes including tumorigenesis, cell survival, and developmental patterning. GSK-3 is constitutively active in non-stimulated cells and can negatively regulate canonical Wnt/-catenin signaling^[2]^[3]. SB-216763 is a maleimide-derived GSK-3 inhibitor with IC50 value of 34nM for GSK-3K (measured by recombinant human GSK-3K). SB-216763 is equally effective at inhibiting GSK-3 and SB-216763<6uM can induce transcription of a-catenin-LEF/TCF regulated reporter gene dose-dependently in serum starved HEK293 for 16h ^[1]. Treatment with 5uM SB-216763 for 4h can increase levels of cytoplasmic-catenin, which is a target negatively regulated by GSK-3, in both serum-starved cerebellar granule neurons and HEK293 cells. SB-216763 (3-5uM) can confer a marked reduction in GSK-3-dependent tau phosphorylation at Ser202-phosphoepitopes in transfected HEK293 cells and endogenous tau protein in cerebellar granule neurons^[4]. SB-216763 can cross the blood–brain barrier and enter the CNS in both rodents and nonhuman primates^[5]. Co-infusion of SB-216763 corrected all responses to Aβ infusion except the induction of gliosis and behavioral deficits in the Morris water maze of rats ^[6].
作用机制Mechanism: SB-216763 can inhibit GSK-3 in an ATP competitive manner. ^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2 μM	12941331
human 5637 cell	-	Growth inhibition assay	-	Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM	SANGER
human A101D cell	-	Growth inhibition assay	-	Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM	SANGER

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6938 mL
- 13.4692 mL
- 26.9384 mL
- 5 mM
- 0.5388 mL
- 2.6938 mL
- 5.3877 mL
- 10 mM
- 0.2694 mL
- 1.3469 mL
- 2.6938 mL

技术信息

CAS号

280744-09-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H12Cl2N2O2

运输

蓝冰

分子量

371.22

别名

SB-216763

溶解度

DMSO	50.0 mg/mL (134.7 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	39 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

HEK293 cells	-	Function assay	-	Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2 μM	12941331
human 5637 cell	-	Growth inhibition assay	-	Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM	SANGER
human A101D cell	-	Growth inhibition assay	-	Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM	SANGER
human A2058 cell	-	Growth inhibition assay	-	Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM	SANGER
human A498 cell	-	Growth inhibition assay	-	Inhibition of human A498 cell growth in a cell viability assay, IC50=19.4549 μM	SANGER
human A704 cell	-	Growth inhibition assay	-	Inhibition of human A704 cell growth in a cell viability assay, IC50=34.2059 μM	SANGER
human AGS cell	-	Growth inhibition assay	-	Inhibition of human AGS cell growth in a cell viability assay, IC50=38.2039 μM	SANGER
human ALL-PO cell	-	Growth inhibition assay	-	Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 μM	SANGER
human BB49-HNC cell	-	Growth inhibition assay	-	Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=44.0278 μM	SANGER
human BE-13 cell	-	Growth inhibition assay	-	Inhibition of human BE-13 cell growth in a cell viability assay, IC50=38.7783 μM	SANGER
human BFTC-905 cell	-	Growth inhibition assay	-	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=21.1879 μM	SANGER
human BHT-101 cell	-	Growth inhibition assay	-	Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=17.6099 μM	SANGER
human BT-549 cell	-	Growth inhibition assay	-	Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 μM	SANGER
human BV-173 cell	-	Growth inhibition assay	-	Inhibition of human BV-173 cell growth in a cell viability assay, IC50=30.7649 μM	SANGER
human BxPC-3 cell	-	Growth inhibition assay	-	Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 μM	SANGER
human CAL-27 cell	-	Growth inhibition assay	-	Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.0054 μM	SANGER
human CAL-72 cell	-	Growth inhibition assay	-	Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=38.1178 μM	SANGER
human Calu-6 cell	-	Growth inhibition assay	-	Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=39.6964 μM	SANGER
human D-423MG cell	-	Growth inhibition assay	-	Inhibition of human D-423MG cell growth in a cell viability assay, IC50=27.9106 μM	SANGER
human D-566MG cell	-	Growth inhibition assay	-	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 μM	SANGER
human DEL cell	-	Growth inhibition assay	-	Inhibition of human DEL cell growth in a cell viability assay, IC50=29.0474 μM	SANGER
human DU-145 cell	-	Growth inhibition assay	-	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 μM	SANGER
human EM-2 cell	-	Growth inhibition assay	-	Inhibition of human EM-2 cell growth in a cell viability assay, IC50=22.6689 μM	SANGER
human ES3 cell	-	Growth inhibition assay	-	Inhibition of human ES3 cell growth in a cell viability assay, IC50=31.3376 μM	SANGER
human ESS-1 cell	-	Growth inhibition assay	-	Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 μM	SANGER
human G-361 cell	-	Growth inhibition assay	-	Inhibition of human G-361 cell growth in a cell viability assay, IC50=10.1798 μM	SANGER
human GAMG cell	-	Growth inhibition assay	-	Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 μM	SANGER
human HDLM-2 cell	-	Growth inhibition assay	-	Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 μM	SANGER
human HepG2 cells	34 μM	Function assay	12 h	Inhibition of GSK3beta in human HepG2 cells assessed as decrease in ratio of phosphorylated GS/GS at 34 uM after 12 hrs by Western blot analysis	25467150
human HMV-II cell	-	Growth inhibition assay	-	Inhibition of human HMV-II cell growth in a cell viability assay, IC50=7.67607 μM	SANGER
human HOP-62 cell	-	Growth inhibition assay	-	Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 μM	SANGER
human HT-29 cell	-	Growth inhibition assay	-	Inhibition of human HT-29 cell growth in a cell viability assay, IC50=27.1752 μM	SANGER
human HuO-3N1 cell	-	Growth inhibition assay	-	Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=22.6151 μM	SANGER
human IGROV-1 cell	-	Growth inhibition assay	-	Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 μM	SANGER
human IST-SL1 cell	-	Growth inhibition assay	-	Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 μM	SANGER
human JAR cell	-	Growth inhibition assay	-	Inhibition of human JAR cell growth in a cell viability assay, IC50=1.21044 μM	SANGER
human K5 cell	-	Growth inhibition assay	-	Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 μM	SANGER
human KOSC-2 cell	-	Growth inhibition assay	-	Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=24.1292 μM	SANGER
human LB2241-RCC cell	-	Growth inhibition assay	-	Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.42874 μM	SANGER
human LoVo cell	-	Growth inhibition assay	-	Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 μM	SANGER
human LS-513 cell	-	Growth inhibition assay	-	Inhibition of human LS-513 cell growth in a cell viability assay, IC50=30.1334 μM	SANGER
human LU-134-A cell	-	Growth inhibition assay	-	Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=31.0238 μM	SANGER
human MIAPaCa2 cells	-	Growth inhibition assay	72 h	Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=25 μM	19338355
human MKN45 cell	-	Growth inhibition assay	-	Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 μM	SANGER
human MKN7 cell	-	Growth inhibition assay	-	Inhibition of human MKN7 cell growth in a cell viability assay, IC50=38.0909 μM	SANGER
human MOLT-4 cell	-	Growth inhibition assay	-	Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=36.1467 μM	SANGER
human MV-4-11 cell	-	Growth inhibition assay	-	Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=2.69685 μM	SANGER
human NB5 cell	-	Growth inhibition assay	-	Inhibition of human NB5 cell growth in a cell viability assay, IC50=11.2157 μM	SANGER
human NB69 cell	-	Growth inhibition assay	-	Inhibition of human NB69 cell growth in a cell viability assay, IC50=26.1764 μM	SANGER
human NBsusSR cell	-	Growth inhibition assay	-	Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=30.5678 μM	SANGER
human NCI-H1770 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1770 cell growth in a cell viability assay. IC50=0.29392 μM	SANGER
human NCI-H1975 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1975 cell growth in a cell viability assay, IC50=32.3582 μM	SANGER
human NCI-H1993 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=8.36534 μM	SANGER
human NCI-H2009 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=13.2427 μM	SANGER
human NCI-H28 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=25.2104 μM	SANGER
human NCI-SNU-1 cell	-	Growth inhibition assay	-	Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=21.5558 μM	SANGER
human NH-12 cell	-	Growth inhibition assay	-	Inhibition of human NH-12 cell growth in a cell viability assay, IC50=28.4059 μM	SANGER
human NKM-1 cell	-	Growth inhibition assay	-	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=23.8512 μM	SANGER
human NMC-G1 cell	-	Growth inhibition assay	-	Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.7264 μM	SANGER
human NY cell	-	Growth inhibition assay	-	Inhibition of human NY cell growth in a cell viability assay, IC50=32.2965 μM	SANGER
human PFSK-1 cell	-	Growth inhibition assay	-	Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=27.593 μM	SANGER
human QIMR-WIL cell	-	Growth inhibition assay	-	Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=15.6394 μM	SANGER
human ReNcell VM cells	3 μM	Proliferation assay	72 h	Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs	20708937
human RPMI-7951 cell	-	Growth inhibition assay	-	Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 μM	SANGER
human RS4-11 cell	-	Growth inhibition assay	-	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 μM	SANGER
human S-117 cell	-	Growth inhibition assay	-	Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 μM	SANGER
human SF539 cell	-	Growth inhibition assay	-	Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM	SANGER
human SK-MEL-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-MEL-1 cell growth in a cell viability, IC50=34.714 μM	SANGER
human SK-MEL-24 cell	-	Growth inhibition assay	-	Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=34.2523 μM	SANGER
human SK-OV-3 cell	-	Growth inhibition assay	-	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.1002 μM	SANGER
human ST14A cells	-	Function assay	6 h	Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis	20708937
human SW1088 cell	-	Growth inhibition assay	-	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=34.3452 μM	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=37.3608 μM	SANGER
human SW1783 cell	-	Growth inhibition assay	-	Inhibition of human SW1783 cell growth in a cell viability assay, IC50=23.5243 μM	SANGER
human SW48 cell	-	Growth inhibition assay	-	Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6067 μM	SANGER
human T47D cell	-	Growth inhibition assay	-	Inhibition of human T47D cell growth in a cell viability assay, IC50=37.1647 μM	SANGER
human T98G cell	-	Growth inhibition assay	-	Inhibition of human T98G cell growth in a cell viability assay, IC50=23.3009 μM	SANGER
human U-266 cell	-	Growth inhibition assay	-	Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 μM	SANGER
human UACC-257 cell	-	Growth inhibition assay	-	Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=27.743 μM	SANGER
human VA-ES-BJ cell	-	Growth inhibition assay	-	Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=22.5763 μM	SANGER
human YH-13 cell	-	Growth inhibition assay	-	Inhibition of human YH-13 cell growth in a cell viability assay, IC50=16.6865 μM	SANGER
mouse 3T3L1 cells	34 μM	Function assay	12 h	Increase in glucose incorporation in mouse 3T3L1 cells at 34 uM after 12 hrs by glucose assay	25467150

3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione Catalog No. CSN12268

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