Art. -Nr.: HY-135825

TFEB activator 1

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC₅₀ of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.

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Reinheit: 99.71%
CAS. Nr.: 39777-61-2
Formel: C₁₉H₁₈O₃
Molecular Weight:294.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years

* The compound is unstable in solutions, freshly prepared is recommended.

TFEB activator 1 Chemical Structure

CAS. Nr.: 39777-61-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 2167 nM (Flag-TFEB nuclear translocation)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	4 μM Compound: GO-Y019	Growth inhibition of human HCT116 cells after 48 hrs by MTS assay Growth inhibition of human HCT116 cells after 48 hrs by MTS assay	[PMID: 20060305]
HeLa	IC₅₀	161 μM Compound: B6	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 19243951]
HL-60	IC₅₀	<12.6 μM Compound: B6	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 19243951]
KB	IC₅₀	<12.6 μM Compound: B6	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 19243951]
MDA-MB-231	GI₅₀	1 μM Compound: 29; GO-Y019	Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by microplate reader analysis Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by microplate reader analysis	[PMID: 32172081]
RPMI-7951	GI₅₀	2.3 μM Compound: 29; GO-Y019	Growth inhibition of human RPMI-7951 cells measured after 72 hrs by microplate reader analysis Growth inhibition of human RPMI-7951 cells measured after 72 hrs by microplate reader analysis	[PMID: 32172081]

In Vitro

TFEB activator 1 (Compound C1) activates TFEB (transcription factor EB) by directly binding to TFEB and promotes its entry into the nucleus, without affecting TFEB phosphorylation or inhibiting the activities of MTOR and MAPK1/ERK2-MAPK3/ERK1^[1].
? TFEB activator 1 (1 μM; for 12 h) significantly increases the levels of LC3B-II, the lipidated and phagophore- or autophagosome-associated form of MAP1LC3B/LC3B (microtubule-associated protein 1 light chain 3 β) in N2a cells^[1].
? TFEB activator 1 (0.2-1 μM) dose-dependently increases the levels of LC3-II and SQSTM1/p62 (sequestosome 1) in N2a cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

N2a cells
Concentration:

0, 0.2, 0.4, 0.6, 0.8 and 1 μM
Incubation Time:

12 hours
Result:

Treatment dose-dependently increased the levels of LC3-II and SQSTM1/p62 (sequestosome 1).

In Vivo

The medium lethal dose (LD₅₀) value of TFEB activator 1 (Compound C1) is 175 mg/kg in the acute toxicity assay (single-dose i.v. tail vein injection; in rats) ^[1].
? Short-term oral administration of TFEB activator 1 (low dosage 10 mg/kg and high dosage 25 mg/kg; for 24 h) dose-dependently increases the expression of LC3B-II and TFEB in the liver, frontal cortex and striatum of the brain^[1].
? Chronic administration of TFEB activator 1 (10 mg/kg per day; orally administered by gavage) activates TFEB and enhances autophagy in rat brains^[1].

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

Animal Model:

Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g^[1]
Dosage:

10 mg/kg and 25 mg/kg
Administration:

Short-term oral administration; for 24 hours
Result:

Activated TFEB and enhanced autophagy and lysosome biogenesis in rat brain.

Animal Model:

Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g^[1]
Dosage:

10 mg/kg
Administration:

Chronic oral administration; daily; for 21 days
Result:

Activated TFEB and enhanced autophagy in rat brains.

Chemical Information

CAS. Nr. 39777-61-2
Appearance Solid
Molecular Weight 294.34
Formel C₁₉H₁₈O₃
Color Light yellow to yellow
SMILES

O=C(/C=C/C1=CC=CC=C1OC)/C=C/C2=CC=CC=C2OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (15)

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Autophagy

High-fat diet exacerbates experimental colitis by inhibiting lysosomal function via the STAT3-TFEB Axis. [Abstract]

2026 May 28:1-24. PMID: 42165414
Cell Commun Signal

Cytoplasmic retention of IRF3 binding Vimentin competitively with ERK1/2 mitigates acute myeloid leukemia through TFEB nuclear translocation. [Abstract]

2026 Apr 28;24(1):347. PMID: 42045951
J Neuroinflammation

Intermittent hypoxia therapy ameliorates beta-amyloid pathology via TFEB-mediated autophagy in murine Alzheimer's disease. [Abstract]

2023 Oct 20;20(1):240. PMID: 37864249

TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240. [Abstract]

TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) reduced Aβ plaques in the mouse brain.

TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240. [Abstract]

TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) reduced Aβ load in the mouse cortex.

TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240. [Abstract]

TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) upregulated the colocalization of Aβ with LC3 as well as the colocalization of LC3 with LAMP1 in PAM.

TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240. [Abstract]

TFEB activator 1 (TA1) (1 μM; 12 h) upregulated the transcription activity of TFEB target genes Lamp1, Vps11, Wipi2, and Vps18 in PAM in vitro.

TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240. [Abstract]

PAMs were fixed and stained with anti-TFEB antibody and DAPI. Nuclear translocation of TFEB was measured by quantifying the intensity of TFEB in DAPI. TFEB activator 1 (TA1) (1 μM; 12 h) upregulated the nuclear levels of TFEB in PAM.
Alzheimers Res Ther

Intermittent hypoxia training enhances Aβ endocytosis by plaque associated microglia via VPS35-dependent TREM2 recycling in murine Alzheimer's disease. [Abstract]

2024 Jun 3;16(1):121. PMID: 38831312
Mol Med

REDD1 deficiency alleviates podocyte PANoptosis and restores autophagy in diabetic kidney disease. [Abstract]

2026 May 21. PMID: 42168844
Aging Cell

TFEB Orchestrates Stress Recovery and Paves the Way for Senescence Induction in Human Dermal Fibroblasts. [Abstract]

2025 May 1:e70083. PMID: 40312996
J Ethnopharmacol

Tripterygium wilfordii protects against an animal model of autoimmune hepatitis. [Abstract]

2023 Jun 12:309:116365. PMID: 36907478
J Agric Food Chem

TFEB Dysfunction Mediates Lysosomal Membrane Permeabilization-Induced Pyroptosis in Deoxynivalenol-Exposed Intestinal Epithelium. [Abstract]

2025 Oct 22. PMID: 41122856
Cell Mol Life Sci

Acetyl-CoA synthetase 2 alleviates brain injury following cardiac arrest by promoting autophagy in brain microvascular endothelial cells. [Abstract]

2025 Apr 17;82(1):160. PMID: 40244361
Int Immunopharmacol

Cathepsin B regulated via TFEB and lysosomal membrane permeabilization in adipose tissue macrophages aggravates obesity-related severe acute pancreatitis. [Abstract]

2026 Jul 1:180:116695. PMID: 42019387
Biochim Biophys Acta Mol Basis Dis

DNMT3B attenuates the development of thoracic aortic aneurysm and dissection by suppressing TFEB-mediated autophagy in vascular smooth muscle cells. [Abstract]

2026 Jun 24;1872(7):168331. PMID: 42342163
Biochim Biophys Acta Mol Basis Dis

TFEB activator protects against ethanol toxicity-induced cardiac injury by restoring mitophagy and autophagic flux. [Abstract]

2025 Mar;1871(3):167668. PMID: 39805395
Ren Fail

TXNIP deficiency attenuates renal fibrosis by modulating mTORC1/TFEB-mediated autophagy in diabetic kidney disease. [Abstract]

2024 Dec;46(1):2338933. PMID: 38616177
Mol Immunol

Compound C1 reduced inflammation and activated autophagy in alveolar macrophages in mice. [Abstract]

2025 Mar 25:181:139-147. PMID: 40138784
bioRxiv

2025 Aug 31.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (424.68 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

3.3974 mL

16.9872 mL

33.9743 mL

5 mM

0.6795 mL

3.3974 mL

6.7949 mL

10 mM

0.3397 mL

1.6987 mL

3.3974 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

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 90% Corn Oil

Solubility: ≥ 6.25 mg/mL (21.23 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 4 mg/mL (13.59 mM); Suspended solution; Need ultrasonic

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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Song JX, et al. A novel curcumin analog binds to and activates TFEB in vitro and in vivo independent of MTOR inhibition. Autophagy. 2016 Aug 2;12(8):1372-89. [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

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3974 mL	16.9872 mL	33.9743 mL	84.9358 mL
	5 mM	0.6795 mL	3.3974 mL	6.7949 mL	16.9872 mL
	10 mM	0.3397 mL	1.6987 mL	3.3974 mL	8.4936 mL
	15 mM	0.2265 mL	1.1325 mL	2.2650 mL	5.6624 mL
	20 mM	0.1699 mL	0.8494 mL	1.6987 mL	4.2468 mL
	25 mM	0.1359 mL	0.6795 mL	1.3590 mL	3.3974 mL
	30 mM	0.1132 mL	0.5662 mL	1.1325 mL	2.8312 mL
	40 mM	0.0849 mL	0.4247 mL	0.8494 mL	2.1234 mL
	50 mM	0.0679 mL	0.3397 mL	0.6795 mL	1.6987 mL
	60 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4156 mL
	80 mM	0.0425 mL	0.2123 mL	0.4247 mL	1.0617 mL
	100 mM	0.0340 mL	0.1699 mL	0.3397 mL	0.8494 mL

Keywords

TFEB activator 1

15 Cited Publications

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TFEB activator 1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TFEB activator 1

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TFEB activator 1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TFEB activator 1

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TFEB activator 1 Related Classifications

HY-135825 Related Classifications