Yuanhuacine (Synonyms: Gnidilatidin)

目录号: HY-N7225 纯度: 95.89%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Yuanhuacine (Gnidilatidin)，一种来自 Daphne genkwa 的达芙烷二萜，是 TNBC 基底样 2 (BL2) 亚型的有效和高选择性抑制剂。Yuanhuacine 可诱导细胞 G2/M 阻滞并具有广泛的抗肿瘤活性。Yuanhuacine 是一种具有口服活性的的 DNA 损伤剂。

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Yuanhuacine Chemical Structure

CAS No. : 60195-70-2

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生物活性
纯度 & 产品资料
参考文献

生物活性

Yuanhuacine (Gnidilatidin), a diterpene from Daphne genkwa, is an effective and highly selective inhibitor of the basal-like 2 (BL2) subtype of TNBC. Yuanhuacine can induce G2/M cell cycle arrest and has broad anti-tumor activity. Yuanhuacine is an orally active DNA damaging agent^[1]^[2]^[3].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	13.11 μM Compound: 12	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 23558238]
B16	IC₅₀	> 30 μM Compound: 3	Cytotoxicity against alpha-MSH stimulated mouse B16 cells after 72 hrs by MTT assay Cytotoxicity against alpha-MSH stimulated mouse B16 cells after 72 hrs by MTT assay	[PMID: 23623417]
B16	IC₅₀	0.16 μM Compound: 3	Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry	[PMID: 23623417]
HCT-116	IC₅₀	22.96 μM Compound: 12	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 23558238]
HeLa	IC₅₀	5.56 μM Compound: 12	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 23558238]
HepG2	IC₅₀	8.04 μM Compound: 12	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 23558238]
HL-60	IC₅₀	26.81 μM Compound: 12	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 23558238]
HT-1080	IC₅₀	2.02 μM Compound: 12	Cytotoxicity against human HT1080 cells after 48 hrs by MTT assay Cytotoxicity against human HT1080 cells after 48 hrs by MTT assay	[PMID: 23558238]
K562	IC₅₀	16.08 μM Compound: 12	Cytotoxicity against human K562 cells after 48 hrs by MTT assay Cytotoxicity against human K562 cells after 48 hrs by MTT assay	[PMID: 23558238]
MCF7	IC₅₀	2.39 μM Compound: 12	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23558238]
MT4	IC₅₀	> 34 nM Compound: 4	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by CellTiter-Glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by CellTiter-Glo assay	[PMID: 32997496]
MT4	CC₅₀	> 6.2 μM Compound: 24	Cytotoxicity against human MT4 cells incubated for 3 days by CellTiter-Glo luminescent assay Cytotoxicity against human MT4 cells incubated for 3 days by CellTiter-Glo luminescent assay	[PMID: 31860304]
RKO	IC₅₀	6.5 μM Compound: 12	Cytotoxicity against human RKO cells after 24 hrs by MTT assay Cytotoxicity against human RKO cells after 24 hrs by MTT assay	[PMID: 32223193]
SW-620	IC₅₀	4.3 μM Compound: 12	Cytotoxicity against human SW620 cells after 24 hrs by MTT assay Cytotoxicity against human SW620 cells after 24 hrs by MTT assay	[PMID: 32223193]
U-937	IC₅₀	11.79 μM Compound: 12	Cytotoxicity against human U937 cells after 48 hrs by MTT assay Cytotoxicity against human U937 cells after 48 hrs by MTT assay	[PMID: 23558238]

体外研究
(In Vitro)

Yuanhuacine (0-100 μM，24-72 h) 抑制 H1993，H358，H460，Calu-1，H1299，A549 细胞增殖，IC₅₀ 为 0.009，16.5，6.2，4.1，4.0，0.03 μM^[1]。
Yuanhuacine (0-1000 nM，24 h) 在 H1993 细胞中抑制 p-AMPK 蛋白水平，下调 mTOR 的激活^[1]。
Yuanhuacine (10-100 nM，0-24 h) 抑制 H1993 细胞迁移^[1]。
Yuanhuacine (0-16 μM，24 h) 抑制 UMUC3，HCT116 细胞增殖，IC₅₀ 为 1.89，14.28 μM^[2]。
Yuanhuacine (2 μM，12 h) 诱导 T24T 和 HCT116 细胞 G2/M 期阻滞^[2]。
Yuanhuacine (0-2 μM，12 h) 通过调节 Sp1 蛋白稳定性，上调 p21 转录和蛋白表达^[2]。

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

Cell Viability Assay^[1]

Cell Line:	H1993 cell
Concentration:	0, 0.00128, 0.0064, 20, 100 μM
Incubation Time:	24, 48, 72 h
Result:	Inhibited cell proliferation in a concentration- and time-dependent manner.

Western Blot Analysis^[1]

Cell Line:	H1993 cell
Concentration:	0, 10, 100, 500, 1000 nM
Incubation Time:	24 h
Result:	Significantly increased p-AMPK protein levels, decreased ACC levels, inhibited the autophosphorylation of mTOR at Ser2481 site, inhibited Akt, PKC-α, Rac1 and F-actin, and activated the cell adhesion molecule E-cadherin expression.

Cell Migration Assay ^[1]

Cell Line:	H1993 cell
Concentration:	10, 100 nM
Incubation Time:	0, 24 h
Result:	Inhibited cell migration in a concentration-dependent manner.

Cell Viability Assay^[2]

Cell Line:	T24T, UMUC3, HCT116
Concentration:	0, 2, 4, 8, 16 μM
Incubation Time:	24 h
Result:	Inhibited cell proliferation in a dose-dependent manner.

Cell Cycle Analysis^[2]

Cell Line:	T24T, HCT116
Concentration:	2 μM
Incubation Time:	12 h
Result:	Induced significant G2/M phase arrest.

Western Blot Analysis^[2]

Cell Line:	T24T, HCT116
Concentration:	0, 1, 2 μM
Incubation Time:	12 h
Result:	Up-regulated the expression of p21 protein, but did not show observable induction of p53 protein expression and p53 protein Ser-15 phosphorylation site.

体内研究
(In Vivo)

Yuanhuacine (0.5-1 mg/kg，口服，每日一次，21 天) 抑制小鼠体内肿瘤增殖^[1]。

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

Animal Model:	H1993 cells implanted xenograft mouse model^[1]
Dosage:	0.5, 1 mg/kg; daily; 21 days
Administration:	Oral
Result:	Inhibited tumor growth by 33.4% and 38.8%, respectively, reduced tumor weight, activated AMPK, and inhibited proliferation biomarkers Ki-67 and PCNA in tumor tissues.

分子量

648.74

Formula

C₃₇H₄₄O₁₀

CAS 号

60195-70-2

性状

固体

颜色

White to off-white

中文名称

芫花酯甲

结构分类

初始来源

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 : 100 mg/mL (154.14 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	1.5414 mL	7.7072 mL	15.4145 mL
5 mM	0.3083 mL	1.5414 mL	3.0829 mL
10 mM	0.1541 mL	0.7707 mL	1.5414 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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.47%

选择批次：

Data Sheet (620 KB) SDS (252 KB)

COA (297 KB) HNMR (248 KB) CNMR (222 KB) RP-HPLC (301 KB) MS (1015 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ji In Kang, et al. Anti-Tumor Activity of Yuanhuacine by Regulating AMPK/mTOR Signaling Pathway and Actin Cytoskeleton Organization in Non-Small Cell Lung Cancer Cells. PLoS One. 2015 Dec 11;10(12):e0144368. [Content Brief]

[2]. Ruowen Zhang, et al. The Chinese herb isolate yuanhuacine (YHL-14) induces G2/M arrest in human cancer cells by up-regulating p21 protein expression through an p53 protein-independent cascade. J Biol Chem. 2014 Mar 7;289(10):6394-403. [Content Brief]

[3]. Charles S Fermaintt, et al. Yuanhuacine Is a Potent and Selective Inhibitor of the Basal-Like 2 Subtype of Triple Negative Breast Cancer with Immunogenic Potential. Cancers (Basel). 2021 Jun 7;13(11):2834. [Content Brief]

Yuanhuacine 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	1.5414 mL	7.7072 mL	15.4145 mL	38.5362 mL
	5 mM	0.3083 mL	1.5414 mL	3.0829 mL	7.7072 mL
	10 mM	0.1541 mL	0.7707 mL	1.5414 mL	3.8536 mL
	15 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5691 mL
	20 mM	0.0771 mL	0.3854 mL	0.7707 mL	1.9268 mL
	25 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5414 mL
	30 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2845 mL
	40 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9634 mL
	50 mM	0.0308 mL	0.1541 mL	0.3083 mL	0.7707 mL
	60 mM	0.0257 mL	0.1285 mL	0.2569 mL	0.6423 mL
	80 mM	0.0193 mL	0.0963 mL	0.1927 mL	0.4817 mL
	100 mM	0.0154 mL	0.0771 mL	0.1541 mL	0.3854 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:

Yuanhuacine60195-70-2Gnidilatidin芫花酯甲DNA/RNA SynthesisOrallyantiproliferativeanti-tumordaphnanediterpenoidInhibitorinhibitorinhibit

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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）

Yuanhuacine (Synonyms: Gnidilatidin)

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