P62-RNF168 agonist-1

目录号: HY-151799 纯度: 98.62%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

P62-RNF168 agonist-1 (compound 5a) 是一种低细胞毒性的 P62-RNF168 激动剂，能促进 P62 与 RNF168 的相互作用。P62-RNF168 agonist-1 诱导 RNF168 介导的 H2A 泛素化减少，并损害同源重组介导的 DNA 修复。P62-RNF168 agonist-1 还能以剂量依赖的方式抑制小鼠异种移植肿瘤的生长。

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P62-RNF168 agonist-1 Chemical Structure

CAS No. : 2765180-17-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3332	In-stock
1 mg	￥1670	In-stock
5 mg	￥3850	In-stock
10 mg	￥5780	In-stock
50 mg		询价
100 mg		询价

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生物活性
纯度 & 产品资料
参考文献

生物活性

P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	1.93 μM Compound: 5a	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
A549	IC₅₀	1.18 μM Compound: 5a	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HCT-116	IC₅₀	0.36 μM Compound: 5a	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HeLa	IC₅₀	2.48 μM Compound: 5a	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HepG2	IC₅₀	19.61 μM Compound: 5a	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MCF-10A	IC₅₀	6.98 μM Compound: 5a	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MCF7	IC₅₀	2.79 μM Compound: 5a	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MDA-MB-231	IC₅₀	1.17 μM Compound: 5a	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MGC-803	IC₅₀	1.88 μM Compound: 5a	Cytotoxicity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
U2OS	IC₅₀	3.64 μM Compound: 5a	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]

体外研究
(In Vitro)

P62-RNF168 agonist-1 (20 μM，72 h) 对癌细胞 HCT116 的 IC₅₀ 为 0.36 μM，对 A549 的 IC₅₀ 为 1.18 μM ，对癌细胞 A357，HeLa，HepG2，MCF-7，MDA-MB-231，MGC-803，H2OS 均具有细胞毒性，不会诱导细胞凋亡，对正常细胞 MCF-10A 毒性较低^[1]。
P62-RNF168 agonist-1 (1-5 μM; 24 h) 影响 HCT-116 细胞中 HR (同源重组) 介导的 DSB 修复发挥抗肿瘤活性^[1]。
P62-RNF168 agonist-1 使 HCT-116 细胞中 P62 和 RNF168 之间的相互作用更加紧密，K _d 为 20.97 μM^[1]。
P62-RNF168 agonist-1 抑制 HCT-116 细胞中 RNF168 的催化活性和 RNF168 E3 连接酶活性^[1]。

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

Cell Proliferation Assay^[1]

Cell Line:	A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells
Concentration:	0-20 µM
Incubation Time:	72 h
Result:	Inhibited A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells, with IC₅₀ values of 1.18, 0.36, 1.93, 2.48, 19.61, 2.79, 1.17, 1.88, 3.64 and 6.98, respectively.

Cell Cycle Analysis^[1]

Cell Line:	HCT-116 cells
Concentration:	1, 2, 5 µM
Incubation Time:	24 h
Result:	Induced a G2/M arrest but no significant accumulation of sub-G1 phase. Compromised both HR(homologous recombination)- and NHEJ (non-homologous end joining)- mediated DSB repair in a dose-dependent manner, but HR was the more severely impacted process.

Western Blot Analysis^[1]

Cell Line:	HCT-116
Concentration:	10 µM
Incubation Time:	Over night
Result:	Had the expression of RNF168 and GST-RNF168 ,increased the level of P62 in the endogenous RNF-168 immune complex.

Apoptosis Analysis^[1]

Cell Line:	HCT-116
Concentration:	5, 10 µM
Incubation Time:	24 h
Result:	Made apoptosis less obvious.

体内研究
(In Vivo)

P62-RNF168 agonist-1 (12.5-100 mg/kg，i.p.，单次剂量) 在 BALB/c 小鼠中的 MTD 为 50 mg/kg，在雌性裸鼠中 MTD 为 12.5 mg/kg^[1]。
Antitumor agent-81 (5-10 mg/kg，i.p.，每三天一次，22 天) 在小鼠中促进肿瘤凋亡，抑制肿瘤生长^[1]。
1.19 P62-RNF168 agonist-1 在雌性裸鼠中的药代动力学^[1].

Dose	T_1/2 (h)	C_max (ng/mL)	AUC_0-t (h?ng/mL)	CL ((mL/h)/kg)
IP (5 mg/kg)	16.17	26.10	215.69	19647.83
IP (10 mg/kg)	31.00	39.87	408.18	16554.30
IP (20 mg/kg)	22.10	52.23	1003.58	14669.81

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

Animal Model:	Female BALB/c nude mice (xenograft tumor model)^[1].
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single every 3 days for 22 days
Result:	Suppressed tumor growth by promoting apoptosis in xenografted tumorigenesis.

Animal Model:	Female BALB/c nude mice^[1].
Dosage:	5, 10, 20 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Exhibited plasma concentration peaked 1 h after administration. Showed a relatively high maximum concentration (C_max= 52.23 ng/mL) and exposure (AUC_0-t= 1003.58 h•ng/mL) at a dose of 20 mg/kg.

Animal Model:	BALB/c mice, Female nude mice^[1]
Dosage:	25, 50, 75, 100 mg/kg, single dose; 12.5, 25, 50 mg/kg, single dose
Administration:	Intraperitoneal injection
Result:	Showed in the 100 mg/kg dosage group of BALB/c mice, out of 8 animals, 3 males and 3 females died on the 7th day, and the remaining animals experienced diarrhea. In the 75 mg/kg dosage group, 1 out of 8 animals (1 male) had diarrhea on the 7th day. There were no deaths or diarrhea observed in the ≤50 mg/kg dosage group. Showed in the female nude mice, both the 25 and 50 mg/kg dosage groups experienced deaths or diarrhea, while the 12.5 mg/kg dosage group had no deaths or diarrhea.

分子量

393.40

Formula

C₁₉H₁₉N₇O₃

CAS 号

2765180-17-2

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 60 mg/mL (152.52 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" 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	2.5419 mL	12.7097 mL	25.4194 mL
5 mM	0.5084 mL	2.5419 mL	5.0839 mL
10 mM	0.2542 mL	1.2710 mL	2.5419 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, 6 months; -20°C, 1 month (protect from light)。-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。

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: ≥ 2.4 mg/mL (6.10 mM); 澄清溶液

此方案可获得 ≥ 2.4 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 24.0 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.4 mg/mL (6.10 mM); 澄清溶液

此方案可获得 ≥ 2.4 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 24.0 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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.4 mg/mL (6.10 mM); 澄清溶液

此方案可获得 ≥ 2.4 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 24.0 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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 98.62%

选择批次：

Data Sheet (643 KB) SDS (251 KB)

COA (194 KB) HNMR (289 KB) RP-HPLC (243 KB) LCMS (101 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wang FC, et al. A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62. J Med Chem. 2022 Nov 4. [Content Brief]

P62-RNF168 agonist-1 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	2.5419 mL	12.7097 mL	25.4194 mL	63.5486 mL
	5 mM	0.5084 mL	2.5419 mL	5.0839 mL	12.7097 mL
	10 mM	0.2542 mL	1.2710 mL	2.5419 mL	6.3549 mL
	15 mM	0.1695 mL	0.8473 mL	1.6946 mL	4.2366 mL
	20 mM	0.1271 mL	0.6355 mL	1.2710 mL	3.1774 mL
	25 mM	0.1017 mL	0.5084 mL	1.0168 mL	2.5419 mL
	30 mM	0.0847 mL	0.4237 mL	0.8473 mL	2.1183 mL
	40 mM	0.0635 mL	0.3177 mL	0.6355 mL	1.5887 mL
	50 mM	0.0508 mL	0.2542 mL	0.5084 mL	1.2710 mL
	60 mM	0.0424 mL	0.2118 mL	0.4237 mL	1.0591 mL
	80 mM	0.0318 mL	0.1589 mL	0.3177 mL	0.7944 mL
	100 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6355 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.

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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。

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P62-RNF168 agonist-1

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