天津泰斯特生化培养箱SPX-150BX

发表于2023年12月20日由上海金畔生物科技有限公司

天津泰斯特生化培养箱SPX-150BX

品牌泰斯特|TAISITE

型号 SPX-150BX

商品详情

天津泰斯特生化培养箱SPX-150BX

产品说明

本产品适用于环境保护、卫生防疫、农畜、药检、水产等科研院校实.验和生产部门，是水体分析和BOD测定细菌、霉菌、微生物的培养、保存、植物栽培、育种实验的专用恒温设备。

产品特征

1、镜面不锈钢工作室。四角呈半圆弧形过渡，易清洁，搁板间距可调。

2、微电脑控制系统，大屏幕液晶显示，具有时间设定、参数记忆、来电恢复功能。

3、品牌压缩机无氟制冷、微风循环。

4、箱体左侧设有φ52mm测试孔，便于测量温度，工作室内仪器与箱体外部标配电源插座的连接。

5、双重密封门结构，内门采用优质钢化玻璃，硅胶条密封，外门采用磁性胶条，启闭方便，密封性好。工作室内设有照明，便于观察。

6、、智能型程序温度湿度控制，可预设30段编程，实现温度的预约定时运行或反复步移，阶梯式的编程运行。

7、、自诊断功能，传感器故障报警、上下限超温报警。

8、、智能制冷化霜系统，保证工作室无霜运行。

9、、自动运行、自动停止、定时运行、来电恢复参数记忆功能、温度显示校正功能。

10、监视计时器、独立式限温器，超过限制温度自动中断输出。

技术参数

型号 Model		电源电压（V） voltage	控温范围（℃） Tem. variation	温度分辨率（℃） Tem.dis- tinguish- ability	恒温波动度（℃） Tem. fluctuation	温度均恒性（℃） Tem.unifor- mity	加热功率 Heat-ing power	制冷剂 Coolant	工作环境温度 Ambienttem.
标准型	SPX-70BⅢ	220V/ 50HZ	0-65℃	0.1℃	±0.5℃	±1℃	300W	R134a	5-30℃
	SPX-150BⅢ						500W
	SPX-250BⅢ						800W
功能型	SPX-70BX						300W
	SPX-150BX						500W
	SPX-250BX						800W

型号 Model		工作室尺寸宽×深×高(mm) Interior dimensions W×D×H	产品外形尺寸宽×深×高(mm) Exterior dimensions W×D×H	包装外形尺寸宽×深×高(mm) Packaging dimensions W×D×H	净重/毛重（kg） Gross/net weight	定时范围 Timing range	载物托板/负荷 Load per rack
标准型	SPX-70BⅢ	420×350×500	570×560×1020	730×720×1170	69/95	1-9999 min	两块（15kg/块） 2pieces (15kg/piece)
	SPX-150BⅢ	500×400×750	640×620×1270	820×760×1430	86/114
	SPX-250BⅢ	500×500×950	600×700×1470	880×825×1645	100/139
功能型	SPX-70BX	420×350×500	570×560×1020	730×720×1170	69/92
	SPX-150BX	500×400×750	640×620×1270	820×760×1430	86/114
	SPX-250BX	500×500×950	600×700×1470	880×825×1645	100/139

性能参数测试在空载条件下为：环境温度20℃，环境湿度50％RH

天津泰斯特生化培养箱SPX-70BX

发表于2023年12月20日由上海金畔生物科技有限公司

天津泰斯特生化培养箱SPX-70BX

品牌泰斯特|TAISITE

型号 SPX-70BX

商品详情

天津泰斯特生化培养箱SPX-70BX

产品说明

产品特征

1、镜面不锈钢工作室。四角呈半圆弧形过渡，易清洁，搁板间距可调。

2、微电脑控制系统，大屏幕液晶显示，具有时间设定、参数记忆、来电恢复功能。

3、品牌压缩机无氟制冷、微风循环。

4、箱体左侧设有φ52mm测试孔，便于测量温度，工作室内仪器与箱体外部标配电源插座的连接。

5、双重密封门结构，内门采用优质钢化玻璃，硅胶条密封，外门采用磁性胶条，启闭方便，密封性好。工作室内设有照明，便于观察。

6、、智能型程序温度湿度控制，可预设30段编程，实现温度的预约定时运行或反复步移，阶梯式的编程运行。

7、、自诊断功能，传感器故障报警、上下限超温报警。

8、、智能制冷化霜系统，保证工作室无霜运行。

9、、自动运行、自动停止、定时运行、来电恢复参数记忆功能、温度显示校正功能。

10、监视计时器、独立式限温器，超过限制温度自动中断输出。

技术参数

型号 Model		电源电压（V） voltage	控温范围（℃） Tem. variation	温度分辨率（℃） Tem.dis- tinguish- ability	恒温波动度（℃） Tem. fluctuation	温度均恒性（℃） Tem.unifor- mity	加热功率 Heat-ing power	制冷剂 Coolant	工作环境温度 Ambienttem.
标准型	SPX-70BⅢ	220V/ 50HZ	0-65℃	0.1℃	±0.5℃	±1℃	300W	R134a	5-30℃
	SPX-150BⅢ						500W
	SPX-250BⅢ						800W
功能型	SPX-70BX						300W
	SPX-150BX						500W
	SPX-250BX						800W

型号 Model		工作室尺寸宽×深×高(mm) Interior dimensions W×D×H	产品外形尺寸宽×深×高(mm) Exterior dimensions W×D×H	包装外形尺寸宽×深×高(mm) Packaging dimensions W×D×H	净重/毛重（kg） Gross/net weight	定时范围 Timing range	载物托板/负荷 Load per rack
标准型	SPX-70BⅢ	420×350×500	570×560×1020	730×720×1170	69/95	1-9999 min	两块（15kg/块） 2pieces (15kg/piece)
	SPX-150BⅢ	500×400×750	640×620×1270	820×760×1430	86/114
	SPX-250BⅢ	500×500×950	600×700×1470	880×825×1645	100/139
功能型	SPX-70BX	420×350×500	570×560×1020	730×720×1170	69/92
	SPX-150BX	500×400×750	640×620×1270	820×760×1430	86/114
	SPX-250BX	500×500×950	600×700×1470	880×825×1645	100/139

性能参数测试在空载条件下为：环境温度20℃，环境湿度50％RH

BX-320

发表于2023年12月8日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BX-320

BX-320 是一种选择性的、ATP 竞争性的、口服有效的直接 PDK1 抑制剂，IC₅₀ 为 30 nM。BX-320 还诱导细胞凋亡 (apoptosis)。具有抗癌作用。

BX-320 Chemical Structure

CAS No. : 702676-93-5

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC₅₀ of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect^[1].

体外研究
(In Vitro)

BX-320 binds to the ATP binding site of PDK1. BX-320 also inhibits Chck1, c-Kit, KDR, PKA, CDK2b/cyclin E, GSK3β, PKC with IC₅₀s of 0.82, 0.89, 1.4, 1.4, 1.5, 4.0, and 5.7 μM, respectively^[1].
BX-320 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis^[1].
BX-320 inhibits the growth of MDA-468 breast cancer cells (IC₅₀=0.6 μM) and induces apoptosis. BX-320 promotes a 12-fold induction of caspase-3/7 activity after 48 h of treatment (IC₅₀=0.5 μm), indicating a strong proapoptotic response^[1].
BX-320 (0.3-10 μM; for 18 hours) greatly reduces the amount of both p-Thr308-Akt and p-Thr386-S6K1^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	MDA-468 breast cancer cells
Concentration:	31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM
Incubation Time:	72 hours
Result:	Blocked the growth of MDA-468 cells (IC₅₀=0.6 μM), which are PTEN-negative breast tumor cells expressing high levels of activated Akt.

Western Blot Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	0, 0.3, 1, 3, 10 μM
Incubation Time:	18 hours
Result:	Reduced the amount of both phospho-Thr³⁰⁸-Akt and phospho-Thr³⁸⁶-S6K1.

体内研究
(In Vivo)

BX-320 (oral dosing with 200 mg/kg, twice a day for 21 days) shows efficacy in a blood-borne metastasis model. BX-320 inhibits the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. BX-320 has efficacy in an in vivo tumor model, which may reflect an inhibition of productive implantation of tumor cells in the lung or an inhibition of subsequent tumor growth^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic (nu/nu) female mice, 6-8 weeks old^[1]
Dosage:	200 mg/kg; dose volume was 10 mL/kg
Administration:	Oral gavage twice daily (12 h apart)
Result:	Significantly inhibited the growth of lung tumors in this model.

分子量

547.45

Formula

C₂₃H₃₁BrN₈O₃

CAS 号

702676-93-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vivo:

1.

BX-320 is dissolved in 20% (w/v) hydroxypropyl-β-cyclodextrin (20 mg/mL) adjusted to pH 4^[1].

参考文献

[1]. Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BX-320

发表于2023年12月8日由上海金畔生物科技有限公司

BX-320

BX-320 是一种选择性的、ATP 竞争性的、口服有效的直接 PDK1 抑制剂，IC₅₀ 为 30 nM。BX-320 还诱导细胞凋亡 (apoptosis)。具有抗癌作用。

BX-320 Chemical Structure

CAS No. : 702676-93-5

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

体外研究
(In Vitro)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	MDA-468 breast cancer cells
Concentration:	31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM
Incubation Time:	72 hours
Result:	Blocked the growth of MDA-468 cells (IC₅₀=0.6 μM), which are PTEN-negative breast tumor cells expressing high levels of activated Akt.

Western Blot Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	0, 0.3, 1, 3, 10 μM
Incubation Time:	18 hours
Result:	Reduced the amount of both phospho-Thr³⁰⁸-Akt and phospho-Thr³⁸⁶-S6K1.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic (nu/nu) female mice, 6-8 weeks old^[1]
Dosage:	200 mg/kg; dose volume was 10 mL/kg
Administration:	Oral gavage twice daily (12 h apart)
Result:	Significantly inhibited the growth of lung tumors in this model.

分子量

547.45

Formula

C₂₃H₃₁BrN₈O₃

CAS 号

702676-93-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vivo:

1.

BX-320 is dissolved in 20% (w/v) hydroxypropyl-β-cyclodextrin (20 mg/mL) adjusted to pH 4^[1].

参考文献

[1]. Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BX-320

发表于2023年12月7日由上海金畔生物科技有限公司

BX-320

BX-320 是一种选择性的、ATP 竞争性的、口服有效的直接 PDK1 抑制剂，IC₅₀ 为 30 nM。BX-320 还诱导细胞凋亡 (apoptosis)。具有抗癌作用。

BX-320 Chemical Structure

CAS No. : 702676-93-5

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	MDA-468 breast cancer cells
Concentration:	31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM
Incubation Time:	72 hours
Result:	Blocked the growth of MDA-468 cells (IC₅₀=0.6 μM), which are PTEN-negative breast tumor cells expressing high levels of activated Akt.

Western Blot Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	0, 0.3, 1, 3, 10 μM
Incubation Time:	18 hours
Result:	Reduced the amount of both phospho-Thr³⁰⁸-Akt and phospho-Thr³⁸⁶-S6K1.

体内研究
(In Vivo)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic (nu/nu) female mice, 6-8 weeks old^[1]
Dosage:	200 mg/kg; dose volume was 10 mL/kg
Administration:	Oral gavage twice daily (12 h apart)
Result:	Significantly inhibited the growth of lung tumors in this model.

分子量

547.45

Formula

C₂₃H₃₁BrN₈O₃

CAS 号

702676-93-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vivo:

1.

BX-320 is dissolved in 20% (w/v) hydroxypropyl-β-cyclodextrin (20 mg/mL) adjusted to pH 4^[1].

参考文献

[1]. Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BX795

发表于2023年10月31日由上海金畔生物科技有限公司

BX795 纯度: 99.17%

BX795 是一种有效的、选择性的 PDK1 抑制剂，IC₅₀ 值为 6 nM。同时，BX795 为有效、相对特异性的TBK1 和 IKKɛ 的抑制剂，IC₅₀ 值分别为 6 和 41 nM。BX795 抑制 S6K1，Akt，PKCδ 和 GSK3β 的磷酸化。BX795 对 PKA，PKC，c-Kit，GSK3β 选择性较低。BX795 可调节自噬 (autophagy)。

BX795 Chemical Structure

CAS No. : 702675-74-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥781	In-stock
5 mg	￥600	In-stock
10 mg	￥1100	In-stock
25 mg	￥2400	In-stock
50 mg	￥3900	In-stock
100 mg	￥6200	In-stock
200 mg	￥9900	In-stock
500 mg		询价
1 g		询价

* Please select Quantity before adding items.

BX795 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
NF-κB Signaling Compound Library
PI3K/Akt/mTOR Compound Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[2]

PDK1

6 nM (IC₅₀)

TBK1

6 nM (IC₅₀)

IKKε

41 nM (IC₅₀)

体外研究
(In Vitro)

BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC₅₀ of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC₅₀ of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively^[1]. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β^[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

591.47

Formula

C₂₃H₂₆IN₇O₂S

CAS 号

702675-74-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (56.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6907 mL	8.4535 mL	16.9070 mL
5 mM	0.3381 mL	1.6907 mL	3.3814 mL
10 mM	0.1691 mL	0.8454 mL	1.6907 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

[2]. Clark K, et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem. 2009 May 22;284(21):141

[3]. Dangelmaier C, et al. PDK1 selectively phosphorylates Thr(308) on Akt and contributes to human platelet functional responses. Thromb Haemost. 2014 Mar 3;111(3):508-17.

Kinase Assay ^[1]	PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average±S.E. of two or more replicates. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. [2]. Clark K, et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem. 2009 May 22;284(21):141 [3]. Dangelmaier C, et al. PDK1 selectively phosphorylates Thr(308) on Akt and contributes to human platelet functional responses. Thromb Haemost. 2014 Mar 3;111(3):508-17.

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BX-912

发表于2023年10月9日由上海金畔生物科技有限公司

BX-912 纯度: 99.53%

BX-912 是一种直接的，选择性的，ATP 竞争性的 PDK1 抑制剂 (IC₅₀=26 nM)。BX-912 阻断肿瘤细胞 PDK1/Akt 信号转导，抑制多种肿瘤细胞株的锚定依赖性生长或诱导凋亡。

BX-912 Chemical Structure

CAS No. : 702674-56-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1382	In-stock
5 mg	￥1256	In-stock
50 mg	￥5022	In-stock
100 mg	￥7533	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BX-912 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC₅₀=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis^[1].

IC₅₀ & Target

IC50: 26 nM (PDK1)^[1]

体外研究
(In Vitro)

BX-912 promotes a block at the G2/M phase of the cell cycle in MDA-468 cells^[1].
BX-912 binds to the ATP binding site of PDK1, and is 9-fold selective for PDK1 relative to PKA. BX-912 blocks PDK1 activity in PTEN-negative PC-3 cells. PTEN-negative PC-3 cells display constitutive activation of Akt which is reflected in high levels of the PDK1 product, phospho-Thr³⁰⁸-Akt^[1].
BX-912 is identified in a coupled assay measuring PDK1- and PtdIns-3,4-P₂-mediated Akt activation, which can detect inhibitors of PDK1, AKT2, or other steps critical for activation of AKT2^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

471.35

Formula

C₂₀H₂₃BrN₈O

CAS 号

702674-56-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (212.16 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1216 mL	10.6078 mL	21.2157 mL
5 mM	0.4243 mL	2.1216 mL	4.2431 mL
10 mM	0.2122 mL	1.0608 mL	2.1216 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

Kinase Assay ^[1]	PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1 and PtdIns-3,4-P₂ mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contains: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-³³P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P₂-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on Streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay can sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The cell lines MDA-468, MDA-453, HCT-116, U87-MG, U2OS, PC-3, B16F10, and MiaPaCa; LOX amelanotic human melanoma cells; and HeLa cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of BX-912 (1, 10, 100 and 1000 nM) in 1% DMSO and growth medium (final concentration of DMSO, 0.1%), followed by brief shaking. Treated cells are incubated for 72 h, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.

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BX517

发表于2023年7月23日由上海金畔生物科技有限公司

BX517 纯度: ≥98.0%

BX517 是一种有效的，选择性的 PDK1 抑制剂，IC₅₀ 值为 6 nM。

BX517 Chemical Structure

CAS No. : 850717-64-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
5 mg	￥800	In-stock
10 mg	￥1100	In-stock
25 mg	￥1900	In-stock
50 mg	￥3500	In-stock
100 mg	￥5500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BX517 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

BX517 is a potent and selective inhibitor of PDK1 with IC₅₀ of 6 nM.

IC₅₀ & Target

IC50: 6 nM (PDK1)

体外研究
(In Vitro)

BX-517 blocks activation of Akt in tumor cells, is potent with IC₅₀ of 0.1-1.0 μM^[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

282.30

Formula

C₁₅H₁₄N₄O₂

CAS 号

850717-64-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 27 mg/mL (95.64 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5423 mL	17.7117 mL	35.4233 mL
5 mM	0.7085 mL	3.5423 mL	7.0847 mL
10 mM	0.3542 mL	1.7712 mL	3.5423 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (8.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.86 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25.

[2]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

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BX517

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