BIO

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

目錄號：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，無細胞試驗中作用于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 Tyk2 的IC50值為30 nM。BIO 可在人類黑色素瘤細胞中誘導凋亡。

BIO Chemical Structure

CAS: 667463-62-9

規(guī)格	價格	庫存
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	GSK-3α GSK-3β	點擊展開
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	點擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細胞周期化合物庫 NF-κB信號通路庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

BIO是第一個維持人類和小鼠的胚胎干細胞自我更新的藥理劑。

靶點

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)	點擊更多
5 nM	30 nM	0.08 μM	0.30 μM	0.32 μM	點擊更多

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特異性位點磷酸化。^[1]BIO作用于人類和小鼠胚胎干細胞，保持未分化表型，并維持多能狀態(tài)特異性的轉(zhuǎn)錄表達因子Oct-3/4, Rex-1 和 Nanog表達。BIO-介導的Wnt信號激活是功能可逆的，撤掉化合物后，導致人類和小鼠胚胎干細胞的正常多元分化程序。^[2]BIO促進哺乳動物心肌細胞增殖。^[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，且誘導人類黑色素瘤細胞凋亡。^[4]
激酶實驗	激酶實驗
激酶實驗	在Buffer A 或 C中在30°C下進行激酶活性檢測，ATP 終濃度為15 μM。減去空白值，活性計算為在10分鐘溫育期間滲透的皮摩爾磷酸鹽。使用適當?shù)腄MSO稀釋液作為對照。在一些情況下通過SDS-PAGE后放射自顯影測評底物的磷酸化。通過親和層析法，從豬腦中純化GSK-3α/β。檢測中, 在15 μM[γ-³²P] ATP (3,000 Ci/mmol;1 mCi/ml) 存在時，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，終體積為30 μl。在30°C下溫育30分鐘后，25 μl上清液等分試樣點樣到2.5×3 cm Whatman P81磷酸纖維素紙片上，20秒后，過濾器在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，對濕的過濾器進行計數(shù)。
細胞實驗	細胞系	COS1, Hepa 或 SH-SY5Y 細胞
	濃度	~10 μM
	孵育時間	12 或 24 小時
	方法	COS1, Hepa (野生型, CEM/LM AhR 缺陷和 ELB1 ARNT 缺陷), 或 SH-SY5Y細胞在6 cm 培養(yǎng)皿中生長，培養(yǎng)基為含10％胎牛血清的DMEM培養(yǎng)基。當細胞密度達到?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(SH-SY5Y) 或24小時后使用裂解緩沖液(1% SDS, 1 mM原釩酸鈉, 10 mM Tris [pH 7.4])裂解仍在實驗板上的細胞。裂解液通過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。增強的化學發(fā)光是用于檢測。使用如下一抗：小鼠anti-β-catenin CT(識別總β-catenin), 小鼠anti-phospho-β-catenin(識別去磷酸化的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。
實驗圖片	檢測方法	檢測指標	實驗圖片	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。^[4]
動物實驗	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
[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

參考文獻

[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

化學信息&溶解度

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

體外溶解度
批次：

DMSO : 71 mg/mL ( (199.34 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 6 mg/mL (16.84 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

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

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

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

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(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：如該濃度超過該批次藥物DMSO溶解度，請先聯(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。

技術(shù)支持

在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。

操作手冊

如果有其他問題，請給我們留言。

* 必填項

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):

成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

BIO