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
CAS: 667463-62-9
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 |
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| 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) | |||
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体外溶解度 |
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 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
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
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
%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，注：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：取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：取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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