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SU056

Alias: SU056; SU-056
Cat No.:V35248 Purity: ≥98%
SU056 is a YB-1 inhibitor.
SU056
SU056 Chemical Structure CAS No.: 2376580-08-2
Product category: Others 11
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: =99.89%

Product Description
SU056 is a YB-1 inhibitor. SU056 induces cycle arrest and apoptosis in ovarian cancer cells, and inhibits cell migration of ovarian cancer cells. SU056 interacts with YB-1 and inhibits its associated downstream proteins and pathways. SU056 enhances the cytotoxic effects of paclitaxel .
SU056 (CAS#: 2376580-08-2) is a YB-1 (Y box binding protein 1) inhibitor. It induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits its associated downstream proteins and pathways. It also enhances the cytotoxic effect of paclitaxel, making it a potential combination therapy for ovarian cancer.
Biological Activity I Assay Protocols (From Reference)
Targets
YB-1[1]
SU056 targets Y box binding protein 1 (YB-1), a multifunctional protein that regulates transcription and translation and is involved in cancer progression. It inhibits YB-1 with an IC50 of 1.73 μM in SKOV3 cells. By inhibiting YB-1, SU056 disrupts downstream signaling pathways involved in cell proliferation, survival, and migration.
ln Vitro
SU056 (between 0 and 10 μM, for 48 hours) stops OVCAR3/4/5/8, SKOV3, and ID8 cells from growing [1]. OVCAR-8 and ID8 cell colony formation is dose-dependently inhibited by SU056 (1 μM, 5-8 days) [1]. OVCAR8, SKOV3, and ID8 cells are arrested in sub-G1 and G1 phases by SU056 (1–5 μM, 6 hours) [1]. OVCAR8, SKOV3, and ID8 cell migration is inhibited by SU056 (0-1 μM, 12 hours) [1]. OVCAR8, SKOV3, and ID8 cells undergo apoptosis in response to SU056 (0–5 μM, 24 h) [1]. In OVCAR8 cells, SU056 (1–5 μM, 12 h) suppresses the production of PMSB2, SUMO2, YB-1, and TMSB10 proteins [1]. Paclitaxel (HY-B0015) (0.1, 0.5, and 1 nM) had its cytotoxic effects enhanced by SU056 (0.1, 0.5, and 1 μM, 48 hours)[1].
In vitro, SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. It interacts with YB-1 and inhibits its associated downstream proteins and pathways. The compound enhances the cytotoxic effect of paclitaxel, suggesting a potential role in combination therapy. Its IC50 in SKOV3 cells is 1.73 μM.
ln Vivo
In mice implanted with ID8 cells, SU056 (20 mg/kg, i.p.) reduces the formation of tumors [1]. In immunodeficient mice implanted with ovarian cancer cells (OVCAR8), SU056 (10 mg/kg, intraperitoneal injection, daily) in combination with Paclitaxel (5 mg/kg, intraperitoneal injection, weekly) inhibits tumor growth, and the effect is more evident than administration alone [1].
In vivo data for SU056 are limited. As a YB-1 inhibitor, it is expected to have potential for cancer therapy. However, specific in vivo studies have not been detailed in the available literature. Further research is needed to evaluate its efficacy and safety in animal models of ovarian cancer.
Enzyme Assay
The in vitro binding assay for SU056 involves measuring its interaction with YB-1. This can be done using surface plasmon resonance (SPR) or pull-down assays. The compound's IC50 of 1.73 μM in SKOV3 cells was determined using cell-based assays. These assays confirm its mechanism of action as a YB-1 inhibitor.
Cell Assay
Cell Viability Assay[1]
Cell Types: OVCAR3/4/5/8, SKOV3 and ID8 cells
Tested Concentrations: 0-10 μM approximately
Incubation Duration: 48 h
Experimental Results: Inhibited cell growth with IC50 values of 1.27, 6.8, 4.33, 3.18, 1.73, 3.75 μM.
Cell Migration Assay [1]
Cell Types: OVCAR8, SKOV3, and ID8 cells
Tested Concentrations: 0, 0.5, 1 μM
Incubation Duration: 12 h
Experimental Results: Dose-dependently inhibited cell migration.
Western Blot Analysis[1]
Cell Types: OVCAR8 cell
Tested Concentrations: 1-5 μM
Incubation Duration: 12 h
Experimental Results: Dose- dependently inhibited the YB-1, TMSB10, SUMO2, and PMSB2 proteins.
Cellular assays for SU056 are performed using ovarian cancer cell lines, such as SKOV3. Cells are treated with varying concentrations of the compound, and cell cycle distribution, apoptosis, and cell migration are assessed. The compound's ability to inhibit YB-1 and its downstream pathways is confirmed by Western blotting.
Animal Protocol
Animal/Disease Models: C57BL/6 mice implanted (sc) with luciferase-expressing ID8 cells[1]
Doses: 20 mg/kg
Route of Administration: intraperitoneal (ip)injection
Experimental Results: diminished the tumor weight by 2-fold, and is well-tolerated. diminished the lung metastases. Inhibited YB-1 expression and downstream MDR1 (IHC assay of tumor sample).
In vivo animal protocols for SU056 are not available in the literature. As a YB-1 inhibitor, it would typically be evaluated in mouse xenograft models of ovarian cancer. However, such studies have not been reported. The compound is currently used primarily for in vitro research.
ADME/Pharmacokinetics
Pharmacokinetic (PK) properties of SU056 have not been characterized. It is a small molecule with a molecular weight of 369.34. The compound is typically dissolved in DMSO for in vitro studies. Further studies are needed to determine its oral bioavailability, half-life, and tissue distribution.
Toxicity/Toxicokinetics
Toxicity data for SU056 are limited. As a YB-1 inhibitor, it may have on-target toxicities related to the essential role of YB-1 in normal cells. The compound is intended for research use only and is not approved for human therapeutic use. Comprehensive toxicological studies are needed.
References

[1]. Y box binding protein 1 inhibition as a targeted therapy for ovarian cancer. Cell Chem Biol. 2021 Aug 19;28(8):1206-1220.e6.

[2]. Inhibition of protein translational machinery in triple-negative breast cancer as a promising therapeutic strategy. Cell Rep Med. 2024 May 21;5(5):101552.

Additional Infomation
SU056 is a YB-1 inhibitor that induces cell-cycle arrest, apoptosis, and inhibits migration in ovarian cancer cells. It enhances the cytotoxic effect of paclitaxel. The compound is used as a research tool for studying YB-1 biology and is not currently in clinical trials.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H16FNO5
Molecular Weight
369.343149185181
Exact Mass
369.101
CAS #
2376580-08-2
PubChem CID
155351586
Appearance
White to off-white solid powder
LogP
2.3
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
3
Heavy Atom Count
27
Complexity
640
Defined Atom Stereocenter Count
0
SMILES
N1(CCO)C2C(=CC3OCOC=3C=2)C(C2=CC=CC(F)=C2)C2C(=O)OCC1=2
InChi Key
WVJVLSHRAJOEEW-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H16FNO5/c21-12-3-1-2-11(6-12)18-13-7-16-17(27-10-26-16)8-14(13)22(4-5-23)15-9-25-20(24)19(15)18/h1-3,6-8,18,23H,4-5,9-10H2
Chemical Name
8-(3-fluorophenyl)-2-(2-hydroxyethyl)-5,12,14-trioxa-2-azatetracyclo[7.7.0.03,7.011,15]hexadeca-1(16),3(7),9,11(15)-tetraen-6-one
Synonyms
SU056; SU-056
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 50 mg/mL (135.38 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (6.77 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 5 mg/mL (13.54 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7075 mL 13.5377 mL 27.0753 mL
5 mM 0.5415 mL 2.7075 mL 5.4151 mL
10 mM 0.2708 mL 1.3538 mL 2.7075 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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