BIO

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

目錄號(hào)：S7198 Purity: 99.9%

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052)是一種特異性的GSK-3抑制劑，無(wú)細(xì)胞試驗(yàn)中作用于GSK-3α/β的IC50為5 nM，比作用于CDK5選擇性高16倍以上，也是一種泛JAK抑制劑，對(duì) Tyk2 的IC50值為30 nM。BIO 可在人類(lèi)黑色素瘤細(xì)胞中誘導(dǎo)凋亡。

BIO Chemical Structure

CAS: 667463-62-9

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1286.64	現(xiàn)貨
10mg	1206.72	現(xiàn)貨
50mg	4671.57	現(xiàn)貨
1g	24488.1	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

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

99.9

BIO相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	GSK-3α GSK-3β	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	Laduviglusib (CHIR-99021) Laduviglusib (CHIR-99021) HCl SB216763 TWS119 CHIR-98014 LY2090314 Tideglusib SB415286 AR-A014418 1-Azakenpaullone IM-12 CP21R7 TDZD-8 Indirubin?(NSC 105327) AZD2858 AZD1080 BIO-acetoxime Bikinin	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) 凋亡分子化合物庫(kù) 細(xì)胞周期化合物庫(kù) NF-κB信號(hào)通路庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

BIO是第一個(gè)維持人類(lèi)和小鼠的胚胎干細(xì)胞自我更新的藥理劑。

靶點(diǎn)

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)	點(diǎn)擊更多
5 nM	30 nM	0.08 μM	0.30 μM	0.32 μM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	BIO (6-bromoindirubin-3'-oxime)是特異性的GSK-3抑制劑，作用于GSK-3α/β，IC50為5 nM，比作用于CDK5選擇性高16倍以上。BIO與這些激酶的ATP結(jié)合口袋相互作用，降低β-catenin在GSK-3特異性位點(diǎn)磷酸化。^[1]BIO作用于人類(lèi)和小鼠胚胎干細(xì)胞，保持未分化表型，并維持多能狀態(tài)特異性的轉(zhuǎn)錄表達(dá)因子Oct-3/4, Rex-1 和 Nanog表達(dá)。BIO-介導(dǎo)的Wnt信號(hào)激活是功能可逆的，撤掉化合物后，導(dǎo)致人類(lèi)和小鼠胚胎干細(xì)胞的正常多元分化程序。^[2]BIO促進(jìn)哺乳動(dòng)物心肌細(xì)胞增殖。^[3] BIO也是pan-JAK抑制劑，作用于TYK2, JAK1, JAK2 和 JAK3，IC50值分別為0.03, 1.5, 8.0, 0.5 μM。BIO選擇性抑制STAT3磷酸化，且誘導(dǎo)人類(lèi)黑色素瘤細(xì)胞凋亡。^[4]
激酶實(shí)驗(yàn)	激酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	在Buffer A 或 C中在30°C下進(jìn)行激酶活性檢測(cè)，ATP 終濃度為15 μM。減去空白值，活性計(jì)算為在10分鐘溫育期間滲透的皮摩爾磷酸鹽。使用適當(dāng)?shù)腄MSO稀釋液作為對(duì)照。在一些情況下通過(guò)SDS-PAGE后放射自顯影測(cè)評(píng)底物的磷酸化。通過(guò)親和層析法，從豬腦中純化GSK-3α/β。檢測(cè)中, 在15 μM[γ-³²P] ATP (3,000 Ci/mmol;1 mCi/ml) 存在時(shí)，含5 μl 40 μM GS-1肽, 一種特異性GSK-3底物(YRRAAVPPSPSLSRHSSPHQSpEDEEE)的1 mg BSA/ml 10 mM DTT在buffer A中按1/100稀釋?zhuān)K體積為30 μl。在30°C下溫育30分鐘后，25 μl上清液等分試樣點(diǎn)樣到2.5×3 cm Whatman P81磷酸纖維素紙片上，20秒后，過(guò)濾器在10 ml磷酸/升水的溶液中洗滌5次（每次至少5分鐘）。在1 ml ACS閃爍液存在時(shí)，對(duì)濕的過(guò)濾器進(jìn)行計(jì)數(shù)。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	COS1, Hepa 或 SH-SY5Y 細(xì)胞
	濃度	~10 μM
	孵育時(shí)間	12 或 24 小時(shí)
	方法	COS1, Hepa (野生型, CEM/LM AhR 缺陷和 ELB1 ARNT 缺陷), 或 SH-SY5Y細(xì)胞在6 cm 培養(yǎng)皿中生長(zhǎng)，培養(yǎng)基為含10％胎牛血清的DMEM培養(yǎng)基。當(dāng)細(xì)胞密度達(dá)到?70％匯合上，IO (5 μM), BIO (5 或 10 μM), MeBIO (5或50 μM), LiCl (20或40 mM), 或模擬液 (DMSO, 終濃度為0.5% )加入到培養(yǎng)基中。12 小時(shí)(SH-SY5Y) 或24小時(shí)后使用裂解緩沖液(1% SDS, 1 mM原釩酸鈉, 10 mM Tris [pH 7.4])裂解仍在實(shí)驗(yàn)板上的細(xì)胞。裂解液通過(guò)26G針頭數(shù)次，在10,000×g下離心5分鐘，調(diào)整到相等蛋白質(zhì)濃度。上樣約8 μg每種樣品，用于免疫印跡分析。增強(qiáng)的化學(xué)發(fā)光是用于檢測(cè)。使用如下一抗：小鼠anti-β-catenin CT(識(shí)別總β-catenin), 小鼠anti-phospho-β-catenin(識(shí)別去磷酸化的β-catenin), 小鼠anti-GSK-3β, 小鼠anti-GSK-3 phosphoTyr216, 兔anti-AhR(芳香烴受體), 及兔anti-Actin。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	BIO處理小鼠移植瘤模型，抑制黑色素瘤生長(zhǎng)。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	小鼠
	Dosages	50 mg/kg
	Administration	口服飼喂

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
[1] Meijer L, et al. Chem Biol, 2003, 10(12), 1255-1266. [2] Sato N, et al. Nat Med, 2004, 10(1), 55-63. [3] Tseng AS, et al. Chem Biol, 2006, 13(9), 957-963. [4] Liu L, et al. Cancer Res. 2011 Jun 1;71(11):3972-3279. + 展開(kāi)

參考文獻(xiàn)

[1] Meijer L, et al. Chem Biol, 2003, 10(12), 1255-1266.
[2] Sato N, et al. Nat Med, 2004, 10(1), 55-63.
[3] Tseng AS, et al. Chem Biol, 2006, 13(9), 957-963.

[4] Liu L, et al. Cancer Res. 2011 Jun 1;71(11):3972-3279.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	356.17	分子式	C₁₆H₁₀BrN₃O₂
CAS號(hào)	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
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 71 mg/mL ( (199.34 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 6 mg/mL (16.84 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊(cè)

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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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BIO