1. MAPK/ERK Pathway Apoptosis
  2. p38 MAPK Apoptosis Caspase Bcl-2 Family
  3. Vacquinol-1

Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates the MAPK pathway. Vacquinol-1 inhibits the growth, migration and colony formation, and induces apoptosis of cancer cells. Vacquinol-1 is applicable to research related to cancers such as hepatocellular carcinoma.

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

Vacquinol-1

Vacquinol-1 Chemical Structure

CAS No. : 5428-80-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates the MAPK pathway. Vacquinol-1 inhibits the growth, migration and colony formation, and induces apoptosis of cancer cells. Vacquinol-1 is applicable to research related to cancers such as hepatocellular carcinoma[1][2].

Cellular Effect
Cell Line Type Value Description References
U3013MG IC50
3.14 μM
Compound: 1
Cytotoxicity against patient-derived U3013MG cells assessed as reduction in cell viability by Celltiter-Glo reagent based assay
Cytotoxicity against patient-derived U3013MG cells assessed as reduction in cell viability by Celltiter-Glo reagent based assay
[PMID: 27607569]
In Vitro

Vacquinol-1 (1.56-25 μM; 24-72 h) inhibits the viability of BEL7402/Huh7 hepatocellular carcinoma cells in vitro[1].
Vacquinol-1 (0-24 μM; 24 h) inhibits the colony-forming ability of BEL7402/Huh7 hepatocellular carcinoma cells and induces cell apoptosis[1].
Vacquinol-1 (10 μM; 24 h) activates the endogenous apoptotic pathway in BEL7402 hepatocellular carcinoma cells, induces the cleavage of caspase-3, caspase-9 and PARP-1, upregulates the expression of Bax and Bim, and downregulates the expression of Bcl-2[1].
Vacquinol-1 (10 μM; 1-12 h) induces the translocation of the pro-apoptotic protein Bax from the cytoplasm to mitochondria in BEL7402 hepatocellular carcinoma cells[1].
Vacquinol-1 (15 μM; 5 h) activates the JNK and p38 MAPK pathways, upregulates α-SMA, an activation marker of the hepatic stellate cell line HSC-T6, promotes collagen production, and induces phosphorylation of the linker region of Smad2/3[2].

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

Cell Proliferation Assay[1]

Cell Line: BEL7402 (hepatocellular carcinoma, HCC)
Concentration: 1.56 μM, 3.13 μM, 6.26 μM, 12.5 μM, 25 μM
Incubation Time: 24, 48, 72 h
Result: Inhibited BEL7402 cell proliferation in a dose-dependent manner.
Reached half maximal inhibitory concentration (IC50) values of 12.35 μM (24 h), 11.48 μM (48 h), and 10.21 μM (72 h).

Cell Proliferation Assay[1]

Cell Line: Huh7 (hepatocellular carcinoma, HCC)
Concentration: 1.56 μM, 3.13 μM, 6.26 μM, 12.5 μM, 25 μM
Incubation Time: 24, 48, 72 h
Result: Inhibited Huh7 cell proliferation in a dose-dependent manner.
Reached half maximal inhibitory concentration (IC50) values of 6.21 μM (24 h), 5.58 μM (48 h), and 4.89 μM (72 h).

Apoptosis Analysis[1]

Cell Line: BEL7402 (hepatocellular carcinoma, HCC)
Concentration: 10 μM
Incubation Time: 24 h
Result: Increased the percentage of apoptotic cells.
Resulted in nuclear fragmentation and apoptotic body formation in BEL7402 cells, whereas control cells displayed round, normal nuclei.

Western Blot Analysis[2]

Cell Line: rat hepatic stellate HSC-T6 cells
Concentration: 15 μM
Incubation Time: 5 h
Result: Upregulated the protein levels of phosphorylated (P)-JNK1/2 and P-p38 (but not P-ERK1/2) in HSC-T6 cells.
Increased the protein levels of α-SMA, Collagen I, P-Smad2L, and P-Smad3L in HSC-T6 cells.
Molecular Weight

352.86

Formula

C21H21ClN2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1NCCCC1)C2=CC(C3=CC=C(Cl)C=C3)=NC4=CC=CC=C24

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (35.42 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 2.8340 mL 14.1699 mL 28.3399 mL
5 mM 0.5668 mL 2.8340 mL 5.6680 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
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. 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 2.8340 mL 14.1699 mL 28.3399 mL 70.8496 mL
5 mM 0.5668 mL 2.8340 mL 5.6680 mL 14.1699 mL
10 mM 0.2834 mL 1.4170 mL 2.8340 mL 7.0850 mL
15 mM 0.1889 mL 0.9447 mL 1.8893 mL 4.7233 mL
20 mM 0.1417 mL 0.7085 mL 1.4170 mL 3.5425 mL
25 mM 0.1134 mL 0.5668 mL 1.1336 mL 2.8340 mL
30 mM 0.0945 mL 0.4723 mL 0.9447 mL 2.3617 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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Vacquinol-1
Cat. No.:
HY-19345
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