Art. -Nr.: HY-138657

NCGC00378430

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.07%
CAS. Nr.: 920650-00-6
Formel: C₂₂H₂₃N₃O₅S
Molecular Weight:441.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NCGC00378430 Chemical Structure

CAS. Nr.: 920650-00-6

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC₅₀ of 52 μM in the Alphascreen assay^[1].
? NCGC00378430 (20 μM; 3 days) blocks TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD in T47D cells^[1].
? NCGC00378430 (10 μM; 3 days) reverses the Sine oculis homeobox homolog 1 (SIX1)-induced increase in p-SMAD3 and does not alter total E-CAD levels. NCGC00378430 restores membranous E-CAD in MCF7-SIX1 cells, along with inhibiting FN1 expression^[1].
? NCGC00378430 (10 or 20 μM) disrupts SIX1-EYA2 interaction in breast cancer cells (MCF7, T47D, MDA-MB-231 cells)^[1].
? NCGC00378430 (10 μM; for 3 days) partially reverses SIX1-mediated transcriptional and metabolic signatures in MCF7 breast tumor cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

T47D cells
Concentration:

20 μM
Incubation Time:

3 days
Result:

Blocked TGF-β induced activation of p-Smad3, upregulation of FN1, and downregulation of E-CAD.

In Vivo

NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment^[1].
? NCGC00378430 (20 mg/kg; IV) has a T_1/2α of 0.25 hours^[1].

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

Animal Model:

6-8 week old NSG mice with MCF7 tumor cells^[1]
Dosage:

25 mg/kg
Administration:

Local Injection to the site of tumor; every other day; from day 3 until the day 21
Result:

Dramatically decreased distant metastatic burden compared to vehicle treatment.
Had no growth inhibitory effect.

Animal Model:

Mice^[1]
Dosage:

20 mg/kg (Pharmacokinetic Analysis)
Administration:

IV
Result:

Had a T_1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a V_ss of 4.08 L/kg, a C_max of 6703 ng/mL and an AUC of 3234 ng/mL•hr.

Chemical Information

CAS. Nr. 920650-00-6
Appearance Solid
Molecular Weight 441.50
Formel C₂₂H₂₃N₃O₅S
Color White to off-white
SMILES

O=C(NC1=CC=C(OC)C(S(=O)(N2CCOCC2)=O)=C1)C3=CC=CC(N4C=CC=C4)=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

All

Sort by:

Journal Impact Factor

Oncogene

Cooperation between SIX1 and DHX9 transcriptionally regulates integrin-focal adhesion signaling mediated metastasis and sunitinib resistance in KIRC. [Abstract]

2024 Sep;43(39):2951-2969. PMID: 39174859
Int Immunopharmacol

Six1 promotes alveolar epithelium senescence in pulmonary fibrosis through regulating Tp53. [Abstract]

2025 Sep 23:166:115554. PMID: 40991995

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (226.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2650 mL

11.3250 mL

22.6501 mL

5 mM

0.4530 mL

2.2650 mL

4.5300 mL

10 mM

0.2265 mL

1.1325 mL

2.2650 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (5.66 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hengbo Zhou, et al. Identification of a Small-Molecule Inhibitor That Disrupts the SIX1/EYA2 Complex, EMT, and Metastasis. Cancer Res. 2020 Jun 15;80(12):2689-2702. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2650 mL	11.3250 mL	22.6501 mL	56.6251 mL
	5 mM	0.4530 mL	2.2650 mL	4.5300 mL	11.3250 mL
	10 mM	0.2265 mL	1.1325 mL	2.2650 mL	5.6625 mL
	15 mM	0.1510 mL	0.7550 mL	1.5100 mL	3.7750 mL
	20 mM	0.1133 mL	0.5663 mL	1.1325 mL	2.8313 mL
	25 mM	0.0906 mL	0.4530 mL	0.9060 mL	2.2650 mL
	30 mM	0.0755 mL	0.3775 mL	0.7550 mL	1.8875 mL
	40 mM	0.0566 mL	0.2831 mL	0.5663 mL	1.4156 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1325 mL
	60 mM	0.0378 mL	0.1888 mL	0.3775 mL	0.9438 mL
	80 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
	100 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5663 mL

NCGC00378430

2 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

NCGC00378430

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Phosphatase Inhibitor Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NCGC00378430

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NCGC00378430

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Phosphatase Inhibitor Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) NCGC00378430

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NCGC00378430 Related Classifications

HY-138657 Related Classifications