BIO

别名: GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052)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。

BIO Chemical Structure

BIO Chemical Structure

CAS: 667463-62-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1286.64 现货
10mg 1206.72 现货
50mg 4671.57 现货
1g 24488.1 现货
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产品质控

批次: S719803 DMSO]71 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false 纯度: 99.9%
99.9

BIO相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
A549 Function assay 10 uM 15 mins Inhibition of human mPGES1 from human A549 cells assessed as PGE2 at 10 uM after 15 mins by HPLC 24697244
HT22 Function assay 10 uM 24 hrs Inhibition of GSK3-mediated beta casein phosphorylation in mouse HT22 cells at 10 uM after 24 hrs by Western blot analysis in presence of MG132 22998443
HEK293 Function assay 0.5 to 1 uM Inhibition of human GSK3 activity in HEK293 cells containing the Wnt/beta-catenin activated reporter pSuperTOPFLASH (STF293 cells) at 0.5 to 1 uM by Wnt reporter gene assay 24697244
sf9 Function assay 1 uM Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of human N-terminal GST/His6-tagged GSK3beta (M1 to T420 residues) expressed in baculovirus infected sf9 cells at 1 uM using RBER-IRStide as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of recombinant human N-terminal GST-tagged CDK2 (M1 to L298 residues)/Cyclin A2 (M1 to L432 residues) expressed in baculovirus infected sf9 cells at 1 uM using Histone H1 as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of recombinant human N-terminal GST-tagged CDK5 (M1 to P292 residues)/p35NCK (M1 to R307 residues) expressed in baculovirus infected sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of human N-terminal GST/His6-tagged Aurora B (A2 to A344 residues) expressed in sf9 cells at 1 uM using tetra(LRRLSLG) as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of human N-terminal GST/His6-tagged FGFR1 (G400 to R820 residues) expressed in baculovirus infected sf9 cells at 1 uM using Poly(Glu,Tyr)4:1 as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/Cyclin B1 (M1 to V433 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of recombinant human N-terminal GST-tagged CDK2 (M1 to L298 residues)/Cyclin E1 (M1 to A395 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of human N-terminal GST/His6-tagged Aurora A (M1 to S403 residues) expressed in baculovirus infected sf9 cells at 1 uM using tetra(LRRLSLG) as substrate by filter binding assay 28557430
sf9 Function assay 1 uM Inhibition of human N-terminal GST-tagged Aurora B (M1 to S27 residues) expressed in sf9 cells at 1 uM using CDC25C-derived peptide as substrate by filter binding assay 28557430
HuH7 Antiproliferative assay 72 hrs Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay, IC50 = 6.2 μM. 19783149
HL60 Antiproliferative assay 5 days Antiproliferative activity against human HL60 cells after 5 days by MTT assay, IC50 = 5.4 μM. 19783149
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay, IC50 = 5.3 μM. 28743492
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 5.2 μM. 19783149
IMR90 Antiproliferative assay 72 hrs Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay, IC50 = 1.9 μM. 19783149
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 1.3 μM. 19783149
SH-SY5Y Cytotoxicity assay 48 hrs Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS reduction assay, IC50 = 9 μM. 18816110
SH-SY5Y Function assay 48 hrs Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay, IC50 = 9.5 μM. 16854069
SH-SY5Y Function assay 24 hrs Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay, IC50 = 18 μM. 16854069
IMR32 Cytotoxicity assay 48 hrs Cytotoxicity against human IMR32 cells assessed as cell viability after 48 hrs by MTT assay 21802947
SK-N-SH Cytotoxicity assay 48 hrs Cytotoxicity against human SK-N-SH cells assessed as cell viability after 48 hrs by MTT assay 21802947
NB39 Cytotoxicity assay 48 hrs Cytotoxicity against human NB39 cells assessed as cell viability after 48 hrs by MTT assay 21802947
SH-SY5Y Function assay Inhibition of GSK3-mediated beta-casein phosphorylation in human SH-SY5Y cells in presence of MG132 by Western blot analysis, IC50 = 0.29 μM. 18816110
HEI-OC1 Function assay Protection against cisplatin-induced cell death in neonatal mouse HEI-OC1 cells assessed as reduction in caspase-3/7 activity, EC50 = 0.192 μM. 30091915
SH-SY5Y Function assay Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay, IC50 = 10 μM. 16854069
SH-SY5Y Function assay Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay, IC50 = 13 μM. 16854069
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052)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。
特性 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。
靶点
GSK-3 [1]
(Cell-free assay)
TYK2 [4]
(Cell-free assay)
CDK5/p35 [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
点击更多
5 nM 30 nM 0.08 μM 0.30 μM 0.32 μM
体外研究(In Vitro)
体外研究活性 BIO (6-bromoindirubin-3'-oxime)是特异性的GSK-3抑制剂,作用于GSK-3α/β,IC50为5 nM,比作用于CDK5选择性高16倍以上。BIO与这些激酶的ATP结合口袋相互作用,降低β-catenin在GSK-3特异性位点磷酸化。[1]BIO作用于人类和小鼠胚胎干细胞,保持未分化表型,并维持多能状态特异性的转录表达因子Oct-3/4, Rex-1 和 Nanog表达。BIO-介导的Wnt信号激活是功能可逆的,撤掉化合物后,导致人类和小鼠胚胎干细胞的正常多元分化程序。[2]BIO促进哺乳动物心肌细胞增殖。[3] BIO也是pan-JAK抑制剂,作用于TYK2, JAK1, JAK2 和 JAK3,IC50值分别为0.03, 1.5, 8.0, 0.5 μM。BIO选择性抑制STAT3磷酸化,且诱导人类黑色素瘤细胞凋亡。[4]
激酶实验 激酶实验
在Buffer A 或 C中在30°C下进行激酶活性检测,ATP 终浓度为15 μM。减去空白值,活性计算为在10分钟温育期间渗透的皮摩尔磷酸盐。使用适当的DMSO稀释液作为对照。在一些情况下通过SDS-PAGE后放射自显影测评底物的磷酸化。通过亲和层析法,从猪脑中纯化GSK-3α/β。检测中, 在15 μM[γ-32P] ATP (3,000 Ci/mmol;1 mCi/ml) 存在时,含5 μl 40 μM GS-1肽, 一种特异性GSK-3底物(YRRAAVPPSPSLSRHSSPHQSpEDEEE)的1 mg BSA/ml 10 mM DTT在buffer A中按1/100稀释,终体积为30 μl。在30°C下温育30分钟后,25 μl上清液等分试样点样到2.5×3 cm Whatman P81磷酸纤维素纸片上,20秒后,过滤器在10 ml磷酸/升水的溶液中洗涤5次(每次至少5分钟)。在1 ml ACS闪烁液存在时,对湿的过滤器进行计数。
细胞实验 细胞系 COS1, Hepa 或 SH-SY5Y 细胞
浓度 ~10 μM
孵育时间 12 或 24 小时
方法 COS1, Hepa (野生型, CEM/LM AhR 缺陷和 ELB1 ARNT 缺陷), 或 SH-SY5Y细胞在6 cm 培养皿中生长,培养基为含10%胎牛血清的DMEM培养基。当细胞密度达到〜70%汇合上,IO (5 μM), BIO (5 或 10 μM), MeBIO (5或50 μM), LiCl (20或40 mM), 或模拟液 (DMSO, 终浓度为0.5% )加入到培养基中。12 小时(SH-SY5Y) 或24小时后 使用裂解缓冲液(1% SDS, 1 mM原钒酸钠, 10 mM Tris [pH 7.4])裂解仍在实验板上的细胞。裂解液通过26G针头数次,在10,000×g下离心5分钟,调整到相等蛋白质浓度。上样约8 μg每种样品,用于免疫印迹分析。增强的化学发光是用于检测。使用如下一抗:小鼠anti-β-catenin CT(识别总β-catenin), 小鼠anti-phospho-β-catenin(识别去磷酸化的β-catenin), 小鼠anti-GSK-3β, 小鼠anti-GSK-3 phosphoTyr216, 兔anti-AhR(芳香烃受体), 及兔anti-Actin。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-AKT / AKT / p21 / p27 p-β-catenin / β-catenin FoxO3a / FoxO1 / p-FoxO3a / p-FoxO1 27510556
Immunofluorescence pAKT / p21 / p27 TNF-α E-cadherin / Nanog Oct3/4 27510556
Growth inhibition assay Cell proliferation 27510556
体内研究(In Vivo)
体内研究活性 BIO处理小鼠移植瘤模型,抑制黑色素瘤生长。[4]
动物实验 Animal Models 小鼠
Dosages 50 mg/kg
Administration 口服饲喂
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06337422 Not yet recruiting
Healthy Volunteer
International Bio service
September 23 2024 Phase 1
NCT04276857 Not yet recruiting
Locally Advanced Pancreatic Cancer|Irreversible Electroporation
University of Saskatchewan
September 1 2024 Not Applicable
NCT06359041 Not yet recruiting
Generalized Myasthenia Gravis (gMG)
Cabaletta Bio
August 2024 Phase 1|Phase 2

化学信息&溶解度

分子量 356.17 分子式

C16H10BrN3O2

CAS号 667463-62-9 SDF Download BIO SDF
Smiles C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC(=C4)Br)O)N=O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 71 mg/mL ( (199.34 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 6 mg/mL (16.84 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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。

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