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  2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. Yuanhuacine

Yuanhuacine (Gnidilatidin)，一種來自 Daphne genkwa 的達(dá)芙烷二萜，是 TNBC 基底樣 2 (BL2) 亞型的有效和高選擇性抑制劑。Yuanhuacine 可誘導(dǎo)細(xì)胞 G2/M 阻滯并具有廣泛的抗腫瘤活性。Yuanhuacine 是一種具有口服活性的的 DNA 損傷劑。

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Yuanhuacine Chemical Structure

Yuanhuacine Chemical Structure

CAS No. : 60195-70-2

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(In Vitro)

Yuanhuacine (0-100 μM，24-72 h) 抑制 H1993，H358，H460，Calu-1，H1299，A549 細(xì)胞增殖，IC50 為 0.009，16.5，6.2，4.1，4.0，0.03 μM[1]。
Yuanhuacine (0-1000 nM，24 h) 在 H1993 細(xì)胞中抑制 p-AMPK 蛋白水平，下調(diào) mTOR 的激活[1]。
Yuanhuacine (10-100 nM，0-24 h) 抑制 H1993 細(xì)胞遷移[1]。
Yuanhuacine (0-16 μM，24 h) 抑制 UMUC3，HCT116 細(xì)胞增殖，IC50 為 1.89，14.28 μM[2]。
Yuanhuacine (2 μM，12 h) 誘導(dǎo) T24T 和 HCT116 細(xì)胞 G2/M 期阻滯[2]。
Yuanhuacine (0-2 μM，12 h) 通過調(diào)節(jié) Sp1 蛋白穩(wěn)定性，上調(diào) p21 轉(zhuǎn)錄和蛋白表達(dá)[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.
體內(nèi)研究
(In Vivo)

Yuanhuacine (0.5-1 mg/kg，口服，每日一次，21 天) 抑制小鼠體內(nèi)腫瘤增殖[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 號
性狀

固體

顏色

White to off-white

中文名稱

芫花酯甲
結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (154.14 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.47%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Yuanhuacine
目錄號：
HY-N7225
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