2. PROTAC Stem Cell/Wnt TGF-beta/Smad
  3. PROTACs TGF-beta/Smad
  4. ETTAC-2

ETTAC-2 is a LRG1 PROTAC degrader, degrading LRG1 via the ubiquitin-proteasome pathway with a DC50 value of 8.38 μM. ETTAC-2 penetrates damaged renal cells to reduce the extracellular secretion of LRG1. ETTAC-2 effectively inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated extracellular matrix proteins. ETTAC-2 degrades LRG1 within fibrotic kidneys and the efficacy in inhibiting the TGF-β-Smad3 pathway both in vitro and vivo. ETTAC-2 can be used for renal fibrosis research.

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ETTAC-2

ETTAC-2 Chemical Structure

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Based on 1 publication(s) in Google Scholar

ETTAC-2 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

ETTAC-2 is a LRG1 PROTAC degrader, degrading LRG1 via the ubiquitin-proteasome pathway with a DC50 value of 8.38 μM. ETTAC-2 penetrates damaged renal cells to reduce the extracellular secretion of LRG1. ETTAC-2 effectively inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated extracellular matrix proteins. ETTAC-2 degrades LRG1 within fibrotic kidneys and the efficacy in inhibiting the TGF-β-Smad3 pathway both in vitro and vivo. ETTAC-2 can be used for renal fibrosis research[1].

IC50 & Target

LRG1

8.38 μM (DC50)

In Vitro

ETTAC-2 (0-26μM, 1-48 h) induces LRG1 degradation with an DC50 value of 8.38 μM in a time-dependent manner, which degradation can persist for 6 h in HK-2 cells via the ubiquitin-proteasome pathway[1].
ETTAC-2 alleviates cellular fibrosis in vitro by inhibiting the TGF- β-Smad3 pathway in HK-2 cells[1].

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

ETTAC-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: HK-2 cells
Concentration: 0, 1.625, 3.25, 6.5, 8.38, 13 and 26 μM
Incubation Time: 0, 1, 3, 5, 8, 18 and 24 h
Result: Induced LRG1 degradation in a time-dependent manner.
In Vivo

ETTAC-2 (50 mg/kg, i.v., daily for five days) preserves renal tissue structure and function, mitigates renal fibrosis, degrades LRG1 to inhibit the TGF- β-Smad3 pathway with safety profile in unilateral ureteral obstruction mouse model (post-UUO mice)[1].

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

Animal Model: Male C57BL/6 mice (20 g) (reserved unilateral ureteral obstruction) [1]
Dosage: 50 mg/kg
Administration: i.v., daily for five days
Result: Significant reduced BUN and SCR levels.
Displayed similar kidney appearances, with no notable differences.
Effectively reduced the weight increase of the obstructed kidney by 16.6%.
Markedly decreased renal tubular dilatation and vacuolization in tubular epithelial cells caused by UUO.
Revealed approximately a 50% reduction in renal pathological damage.
Revealed a 64.3% reduction in matrix deposition.
Decreased mRNA expression levels of α-SMA, collagen-1A1, and fibronectin by 79.4%, 74.2% and 58%, respectively.
Diminished the expression areas of α-SMA, collagen-1A1, and fibronectin by 64.4%, 73.4%, and 71.9% respectively.
Decreases in α-SMA, collagen-1A1, and fibronectin protein expression by 60.3%, 61.6% and 53.3%, respectively.
Led to a 46.9% decrease in LRG1 overexpressed.
Indicated a 62.9% reduction in LRG1 levels.
Led to a marked reduction in the fluorescent signals and a notable improvement in tubular structure.
Decreased phosphorylated Smad3 levels by 57.1%.
Had no significant impact on their body weight, did not induce notable morphological alterations in major organs (including heart, liver, spleen, and lungs).
Molecular Weight

1891.07

Formula

C83H123N23O26S
Appearance

Solid

Color

White to off-white

Sequence

Lenalidomide-(CC)-Gly-Gly-Glu-Ser-Tyr-Ser-Ala-Lys-His-Arg-Ile-Met-Leu-Thr
Sequence Shortening

Lenalidomide-(CC)-GGESYSAKHRIMLT
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (52.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (1.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5288 mL 2.6440 mL 5.2880 mL
5 mM 0.1058 mL 0.5288 mL 1.0576 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (1.32 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 (1.32 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.94%

SDS (252 KB)

COA (248 KB) LCMS (79 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 0.5288 mL 2.6440 mL 5.2880 mL 13.2200 mL
DMSO 5 mM 0.1058 mL 0.5288 mL 1.0576 mL 2.6440 mL
10 mM 0.0529 mL 0.2644 mL 0.5288 mL 1.3220 mL
15 mM 0.0353 mL 0.1763 mL 0.3525 mL 0.8813 mL
20 mM 0.0264 mL 0.1322 mL 0.2644 mL 0.6610 mL
25 mM 0.0212 mL 0.1058 mL 0.2115 mL 0.5288 mL
30 mM 0.0176 mL 0.0881 mL 0.1763 mL 0.4407 mL
40 mM 0.0132 mL 0.0661 mL 0.1322 mL 0.3305 mL
50 mM 0.0106 mL 0.0529 mL 0.1058 mL 0.2644 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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ETTAC-2 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:

ETTAC-2ETTAC2ETTAC 2PROTACsTGF-beta/SmadTransforming growth factor betarenal cellsTGF-β-Smad3fibrotic kidneysrenal fibrosisInhibitorinhibitorinhibit

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