1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. (Z)-SKI V

(Z)-SKI V 

Cat. No.: HY-12895A Purity: 98.09%
Handling Instructions

(Z)-SKI V a potent, selective Aurora B kinase inhibitor with an IC50 of 0.735 μM and a Kd of 3.06 μM. (Z)-SKI V inhibits Aurora A with an IC50 of 1.34 μM. (Z)-SKI V, a benzofuran derivative, has extensive cytotoxic effects on cancer cell lines.

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

(Z)-SKI V Chemical Structure

(Z)-SKI V Chemical Structure

CAS No. : 927429-51-4

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Description

(Z)-SKI V a potent, selective Aurora B kinase inhibitor with an IC50 of 0.735 μM and a Kd of 3.06 μM. (Z)-SKI V inhibits Aurora A with an IC50 of 1.34 μM. (Z)-SKI V, a benzofuran derivative, has extensive cytotoxic effects on cancer cell lines[1].

IC50 & Target[1]

Aurora B

0.735 μM (IC50)

Aurora B

3.06 μM (Kd)

Aurora A

1.34 μM (IC50)

GSK3B

2.63 μM (IC50)

FLT1

3.7 μM (IC50)

PDGFRA

4.04 μM (IC50)

Aurora C

4.75 μM (IC50)

FLT4

5.19 μM (IC50)

KDR

5.96 μM (IC50)

In Vitro

(Z)-SKI V (compound S6; 5-20 μM; 24 hours) blocks the proliferation and colony formation of cancer cells in a dose-dependent manner in HeLa cells, HepG2 cells[1].
(Z)-SKI V (2-10 μM; 96 hours) has extensive cytotoxic effects on cancer cell lines[1].
(Z)-SKI V (20 μM; 48 hours) significantly increases the percentage of HepG2 cells in the G2/M phase[1].
(Z)-SKI V (5-20 μM; 48 hours) significantly down-regulates the p-histone H3 (Ser10) signals in HeLa cells, SW620 cells and HepG2 cells[1].

Cell Proliferation Assay[1]

Cell Line: HeLa cells and HepG2 cells
Concentration: 5, 10, 20 μM
Incubation Time: 24 hours
Result: Blocked the proliferation and colony formation of cancer cells in a dose-dependent manner in HeLa cells, HepG2 cells.

Cell Cytotoxicity Assay[1]

Cell Line: SW620 cell
Concentration: 2, 5, or 10 μM
Incubation Time: 96 hours
Result: Had extensive cytotoxic effects on cancer cell lines and potently blocked the SW620 cells by 5 μM and 10 μM.

Cell Cycle Analysis[1]

Cell Line: HeLa, SW620 and HepG2 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: Significantly increased the percentage of HepG2 cells in the G2/M phase, and this increase was accompanied by a decrease in the percentage of cells in the G1 phase.

Western Blot Analysis[1]

Cell Line: HeLa and SW620 cells
Concentration: 5, 10, 20 μM
Incubation Time: 48 hours
Result: Significantly down-regulated the p-histone H3 (Ser10) signals in HeLa cells, SW620 cells and HepG2 cells.
In Vivo

(Z)-SKI V (compound S6; 10 or 20 mg/kg; IP; once a day for 14 days) suppresses the growth of QGY-7401 xenograft tumors in vivo[1].

Animal Model: Male BALB/c nude mice (5-6 weeks of age, 20 g) with human liver cancer QGY-7401 tumor[1]
Dosage: 10 or 20 mg/kg
Administration: IP; once a day for 14 days
Result: Suppressed the growth of QGY-7401 xenograft tumors in vivo.
Molecular Weight

254.24

Formula

C₁₅H₁₀O₄

CAS No.

927429-51-4

SMILES

O=C1/C(OC2=CC=CC=C12)=C/C3=CC=C(O)C(O)=C3.[(Z)]

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 : 250 mg/mL (983.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9333 mL 19.6665 mL 39.3329 mL
5 mM 0.7867 mL 3.9333 mL 7.8666 mL
10 mM 0.3933 mL 1.9666 mL 3.9333 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(Z)-SKI VAurora KinasebenzofurancytotoxiccoloncancerSW620liverHepG2cervicalHeLaQGY7401SMMC7721Inhibitorinhibitorinhibit

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(Z)-SKI V
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