1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. NCGC00378430

NCGC00378430 

Cat. No.: HY-138657 Purity: 99.76%
Handling Instructions

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 52 μM in the Alphascreen assay. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and EMT. NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.

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

NCGC00378430 Chemical Structure

NCGC00378430 Chemical Structure

CAS No. : 920650-00-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor with an IC50 of 52 μM in the Alphascreen assay. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and EMT. NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model[1].

In Vitro

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 20μM) 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].

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 T1/2α of 0.25 hours[1].

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 T1/2α of 0.25 hours, a CL of 6.19 L/hr•kg, a Vss of 4.08 L/kg, a Cmax of 6703 ng/mL and an AUC of 3234 ng/mL•hr.
Molecular Weight

441.50

Formula

C₂₂H₂₃N₃O₅S

CAS No.
SMILES

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

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 : 100 mg/mL (226.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

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

NCGC00378430NCGC 00378430NCGC-00378430PhosphataseSIX1EYA2transcriptionalTGF-βEMTbreastcancerp-Smad3FN1E-CADT47DMCF7MDA-MB-231Inhibitorinhibitorinhibit

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Product Name:
NCGC00378430
Cat. No.:
HY-138657
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