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

Yuanhuacine  (Synonyms: Gnidilatidin)

Cat. No.: HY-N7225 Purity: 95.89%
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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.

For research use only. We do not sell to patients.

Yuanhuacine Chemical Structure

Yuanhuacine Chemical Structure

CAS No. : 60195-70-2

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

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].

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]
In Vitro

Yuanhuacine (0-100 μM, 24-72 h) inhibits the proliferation of H1993, H358, H460, Calu-1, H1299 and A549 cells, with IC50 values of 0.009, 16.5, 6.2, 4.1, 4.0 and 0.03 μM[1].
Yuanhuacine (0-1000 nM, 24 h) inhibits the p-AMPK protein levels in H1993 cells and downregulates the activation of mTOR[1].
Yuanhuacine (10-100 nM, 0-24 h) inhibits the migration of H1993 cells[1].
Yuanhuacine (0-16 μM, 24 h) inhibits the proliferation of UMUC3 and HCT116 cells, with IC50 values of 1.89 and 14.28 μM[2].
Yuanhuacine (2 μM, 12 h) induces G2/M phase arrest in T24T and HCT116 cells[2].
Yuanhuacine (0-2 μM, 12 h) upregulates the transcription and protein expression of p21 by regulating the stability of Sp1 protein[2].

MedChemExpress (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.
In Vivo

Yuanhuacine (0.5-1 mg/kg, oral, once daily, 21 days) inhibits tumor proliferation in mice[1].

MedChemExpress (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.
Molecular Weight

648.74

Formula

C37H44O10

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C)=C[C@]2([H])[C@]1(O)[C@H](O)[C@]3(CO)[C@@]([C@]4([H])[C@]25[C@H](C)[C@@H](OC(C6=CC=CC=C6)=O)[C@@]7(C(C)=C)[C@]4([H])O[C@](O5)(/C=C/C=C/CCCCC)O7)([H])O3

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (154.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.47%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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  • 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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