DBeQ (Synonyms: JRF 12)

目录号: HY-15945 纯度: 99.02%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

DBeQ 是一种有效的，选择性的，ATP 竞争性的 p97 抑制剂，对 p97(wt) 和 p97(C522A) 的 IC₅₀ 值分别为 1.5 μM 和 1.6 μM，同时可抑制 Vps4，IC₅₀ 值为 11.5 μM。

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DBeQ Chemical Structure

CAS No. : 177355-84-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥614	In-stock
5 mg	￥558	In-stock
10 mg	￥958	In-stock
25 mg	￥2100	In-stock
50 mg	￥3570	In-stock
100 mg	￥5700	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC₅₀ of 11.5 μM.

IC₅₀ & Target

IC50: 1.5 μM (p97)^[1], 11.5 μM (Vps4)^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	4.72 μM Compound: 3e	Cytotoxicity against human HT-29 cells after 72 hrs by neutral red dye assay Cytotoxicity against human HT-29 cells after 72 hrs by neutral red dye assay	[PMID: 21700369]
HT-29	IC₅₀	4.72 μM Compound: I	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis	[PMID: 35694693]
J774.A1	EC₅₀	0.67 μM Compound: 10	Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/ET/67/L82 infected in mouse J774A1 cells by colorimetric assay Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/ET/67/L82 infected in mouse J774A1 cells by colorimetric assay	[PMID: 24874647]
J774.A1	EC₅₀	1.4 μM Compound: 10	Antileishmanial activity against intracellular amastigote stage of Leishmania amazonensis LV78 infected in mouse J774A1 cells by colorimetric assay Antileishmanial activity against intracellular amastigote stage of Leishmania amazonensis LV78 infected in mouse J774A1 cells by colorimetric assay	[PMID: 24874647]
J774.A1	EC₅₀	5.5 μM Compound: 1	Cytotoxicity against mouse J774A.1 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Cytotoxicity against mouse J774A.1 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 25749014]
J774.A1	EC₅₀	5.5 μM Compound: 10	Cytotoxicity against mouse J774A1 cells after 72 hrs by MTT assay Cytotoxicity against mouse J774A1 cells after 72 hrs by MTT assay	[PMID: 24874647]
MDA-MB-231	IC₅₀	1.79 μM Compound: 3e	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by neutral red dye assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by neutral red dye assay	[PMID: 21700369]
MDA-MB-231	IC₅₀	1.79 μM Compound: I	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis	[PMID: 35694693]
T-24	IC₅₀	5.96 μM Compound: 3e	Cytotoxicity against human T24 cells after 72 hrs by neutral red dye assay Cytotoxicity against human T24 cells after 72 hrs by neutral red dye assay	[PMID: 21700369]
T-24	IC₅₀	5.96 μM Compound: I	Antiproliferative activity against human T24 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis Antiproliferative activity against human T24 cells assessed as inhibition of cell growth incubated for 72 hrs by neutral red dye based spectrophotometric analysis	[PMID: 35694693]

体外研究
(In Vitro)

DBeQ 是一种 ATP 竞争性 p97 抑制剂，对 p97 (wt) 和 p97 (C522A) 的 IC₅₀ 值分别为 1.5 μM 和 1.6 μM。DBeQ 相对于 ATP来说竞争性地抑制 p97，K_i 为 3.2 ± 0.4 μM。DBeQ 抑制 p97 依赖性底物 UbG76V-GFP 的降解，IC₅₀ 值为 2.6 μM。DBeQ (10 μM) 也显著抑制 TCRα-GFP 的降解，诱导 CHOP 但不增加 p21 水平。此外，DBeQ 抑制 MRC-5、Hek293、HeLa 和 RPMI8226 细胞的活力，GI₅₀s 分别为 6.6 ± 2.9、4 ± 0.6、3.1 ± 0.5 和 1.2 ± 0.3^[1]。
DBeQ 通过特异性结合其 D2 结构域 (p97D2) 的 ATP 酶位点，有效抑制 AAA ATP 酶 p97。DBeQ 还抑制 Vps4，IC₅₀ 为 11.5 μM。此外，DBeQ (30 μM) 抑制野生型细胞 (菌株 YLZ0) 的菌丝生长^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

340.42

Formula

C₂₂H₂₀N₄

CAS 号

177355-84-9

性状

固体

颜色

White to off-white

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 35.71 mg/mL (104.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9375 mL	14.6877 mL	29.3755 mL
5 mM	0.5875 mL	2.9375 mL	5.8751 mL
10 mM	0.2938 mL	1.4688 mL	2.9375 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.34 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.34 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.02%

选择批次：

Data Sheet (638 KB) SDS (393 KB)

COA (196 KB) HNMR (271 KB) RP-HPLC (247 KB) LCMS (264 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Chou TF, et al.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. [Content Brief]

[2]. Zhang Y, et al. The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ. Mycopathologia. 2016 Jun;181(5-6):329-39. [Content Brief]

Cell Assay ^[1]	Cells are seeded on a 384-well solid white plate (5,000 cells/well). Cells are transfected with luciferase siRNA or p97 siRNA (10 nM) for 48 h or treated with DBeQ for the indicated amount of time. Caspase-3/7 Glo, caspase-6 Glo, caspase-8 Glo, or caspase-9 Glo is added into each well and mixed by shaking at 500 rpm for 1 min. Luminescence signal is determined after incubation at room temperature for 1 h. Cellular viability is determined with CellTiter-Glo reagent. To determine the IC₅₀ of cellular viability, cells are treated with MG132 or DBeQ at seven concentrations (threefold serial dilutions starting at 33 μM) for 48 h. IC₅₀ values are calculated from fitting the percentage of luminescence signal normalized to DMSO treated cells)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Chou TF, et al.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. [Content Brief] [2]. Zhang Y, et al. The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ. Mycopathologia. 2016 Jun;181(5-6):329-39. [Content Brief]

Cell Assay
^[1]

Cells are seeded on a 384-well solid white plate (5,000 cells/well). Cells are transfected with luciferase siRNA or p97 siRNA (10 nM) for 48 h or treated with DBeQ for the indicated amount of time. Caspase-3/7 Glo, caspase-6 Glo, caspase-8 Glo, or caspase-9 Glo is added into each well and mixed by shaking at 500 rpm for 1 min. Luminescence signal is determined after incubation at room temperature for 1 h. Cellular viability is determined with CellTiter-Glo reagent. To determine the IC₅₀ of cellular viability, cells are treated with MG132 or DBeQ at seven concentrations (threefold serial dilutions starting at 33 μM) for 48 h. IC₅₀ values are calculated from fitting the percentage of luminescence signal normalized to DMSO treated cells)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Chou TF, et al.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. [Content Brief]

[2]. Zhang Y, et al. The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ. Mycopathologia. 2016 Jun;181(5-6):329-39. [Content Brief]

DBeQ 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9375 mL	14.6877 mL	29.3755 mL	73.4387 mL
	5 mM	0.5875 mL	2.9375 mL	5.8751 mL	14.6877 mL
	10 mM	0.2938 mL	1.4688 mL	2.9375 mL	7.3439 mL
	15 mM	0.1958 mL	0.9792 mL	1.9584 mL	4.8959 mL
	20 mM	0.1469 mL	0.7344 mL	1.4688 mL	3.6719 mL
	25 mM	0.1175 mL	0.5875 mL	1.1750 mL	2.9375 mL
	30 mM	0.0979 mL	0.4896 mL	0.9792 mL	2.4480 mL
	40 mM	0.0734 mL	0.3672 mL	0.7344 mL	1.8360 mL
	50 mM	0.0588 mL	0.2938 mL	0.5875 mL	1.4688 mL
	60 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2240 mL
	80 mM	0.0367 mL	0.1836 mL	0.3672 mL	0.9180 mL
	100 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7344 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DBeQ177355-84-9JRF 12JRF12JRF-12p97AutophagyApoptosisVCPCdc48Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

DBeQ (Synonyms: JRF 12)

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献