2. Metabolic Enzyme/Protease
  3. Sialyltransferase
  4. SPP-002

SPP-002 is a ST6GAL1 inhibitor with a human IC50 of 16.7 μM. SPP-002 selectively inhibits N-glycan sialylation over O-glycan sialylation and binds strongly to the enzyme active site. SPP-002 suppresses expression of signaling proteins in the integrin/FAK/paxillin pathway. SPP-002 can be used for the research of triple negative breast cancer metastasis.

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SPP-002

SPP-002 Chemical Structure

CAS No. : 3067911-81-0

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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

SPP-002 Related Antibodies

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Description

SPP-002 is a ST6GAL1 inhibitor with a human IC50 of 16.7 μM. SPP-002 selectively inhibits N-glycan sialylation over O-glycan sialylation and binds strongly to the enzyme active site. SPP-002 suppresses expression of signaling proteins in the integrin/FAK/paxillin pathway. SPP-002 can be used for the research of triple negative breast cancer metastasis[1].

IC50 & Target[1]

ST6Gal

16.7 nM (IC50)

In Vitro

SPP-002 (Compound 2) (50-1000 μM) potently and selectively inhibits human ST6GAL1 with an IC50 of 16.7 μM, while exhibiting minimal activity against rat ST3GAL1 (IC50 > 1000 μM)[1].
SPP-002 (0.5-80 μM) is non-cytotoxic to MDA-MB-231 human triple-negative breast cancer cells at concentrations up to 80 μM[1].
SPP-002 (60 μM; 16 h) inhibits the migration of MDA-MB-231 human triple-negative breast cancer cells in vitro[1].
SPP-002 (60 μM) potently inhibits the invasion of MDA-MB-231 human triple-negative breast cancer cells in vitro, with a more pronounced effect on invasion than migration[1].
SPP-002 (60 μM; 24-48 h) moderately reduces the adhesion of MDA-MB-231 human triple-negative breast cancer cells to collagen IV and fibronectin in vitro, with greater activity than lithocholic acid[1].
SPP-002 (20-80 μM; 48 h) suppresses sialylation of integrin subunits (αv, α5, β1, β3, β4, β5) in MDA-MB-231 human triple-negative breast cancer cells in vitro in a dose-dependent manner[1].
SPP-002 (20-80 μM; 1-18 h) inhibits phosphorylation of FAK and paxillin in MDA-MB-231 human triple-negative breast cancer cells in both time-dependent and dose-dependent manners, while not altering total FAK or paxillin protein levels[1].

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

SPP-002 Related Antibodies

Cell Migration Assay [1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 60 μM
Incubation Time: 16 h
Result: Decreased the migration potential of MDA-MB-231 cells relative to untreated control cells and cells treated with other test compounds.
The anti-migration activity was attributed to ST inhibitory effects rather than inherent cytotoxicity.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 20 μM; 40 μM; 80 μM
Incubation Time: 48 h
Result: Dose-dependently suppressed the sialylation of integrin αv, α5, β1, β3, β4, and β5 subunits.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 20 μM; 40 μM; 80 μM
Incubation Time: 1 h; 2 h; 4 h; 6 h; 8 h; 18 h
Result: Time-dependently suppressed phosphorylation of FAK (Y397, Y576/577) and paxillin (Y118) starting at 2 h post-treatment, with no significant change in total FAK and paxillin protein levels.
Dose-dependently suppressed phosphorylation of FAK (Y397, Y576/577) and paxillin (Y118) after 2 h of treatment, with minimal change in total FAK and paxillin expression.
Molecular Weight

480.74

Formula

C24H41KO5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](CCCOS(=O)(O[K])=O)[C@H]1CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C
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 : ≥ 25 mg/mL (52.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0801 mL 10.4006 mL 20.8013 mL
5 mM 0.4160 mL 2.0801 mL 4.1603 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.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.0801 mL 10.4006 mL 20.8013 mL 52.0032 mL
5 mM 0.4160 mL 2.0801 mL 4.1603 mL 10.4006 mL
10 mM 0.2080 mL 1.0401 mL 2.0801 mL 5.2003 mL
15 mM 0.1387 mL 0.6934 mL 1.3868 mL 3.4669 mL
20 mM 0.1040 mL 0.5200 mL 1.0401 mL 2.6002 mL
25 mM 0.0832 mL 0.4160 mL 0.8321 mL 2.0801 mL
30 mM 0.0693 mL 0.3467 mL 0.6934 mL 1.7334 mL
40 mM 0.0520 mL 0.2600 mL 0.5200 mL 1.3001 mL
50 mM 0.0416 mL 0.2080 mL 0.4160 mL 1.0401 mL
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SPP-002 Related Classifications

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:

SPP-0023067911-81-0SPP002SPP 002Sialyltransferaserat ST3GAL1N-glycan sialylationST6GAL1fibronectinO-glycan sialylationtriple negative breast cancer metastasisMDA-MB-231 human triple-negative breast cancer cellsintegrin/FAK/paxillin pathwayintegrin subunitscollagen IVInhibitorinhibitorinhibit

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