2. Autophagy
  3. Autophagy
  4. Autophagy activator-2

Autophagy activator-2 is a potent autophagy activator with EC50 values of 14.33 μM. Autophagy activator-2 acts as a proteostasis modulator and small-molecule chaperone that upregulates I1061T mutant NPC1 expression and facilitates cholesterol efflux. Autophagy activator-2 reduces lysosomal hydrolase levels. Autophagy activator-2 can be used for the study of Niemann-Pick Type C disease.

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Autophagy activator-2

Autophagy activator-2 Chemical Structure

CAS No. : 1111050-17-9

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Autophagy activator-2 Related Antibodies

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Description

Autophagy activator-2 is a potent autophagy activator with EC50 values of 14.33 μM. Autophagy activator-2 acts as a proteostasis modulator and small-molecule chaperone that upregulates I1061T mutant NPC1 expression and facilitates cholesterol efflux. Autophagy activator-2 reduces lysosomal hydrolase levels. Autophagy activator-2 can be used for the study of Niemann-Pick Type C disease[1].

In Vitro

Autophagy activator-2 (compound 2) induces autophagosome formation in eGFP-LC3 HeLa cells with an EC50 of 14.33 μM, acting as an autophagy activator near its EC50 and a late-stage inhibitor at higher concentrations[1].
Autophagy activator-2 (20, 40 μM; 6 h in HeLa cells; 20 μM; 24 h in fibroblasts) slightly reduces lysosomal proteolytic activity in wild-type HeLa cells at 20 and 40 μM but significantly enhances proteolytic activity in NPC1I1061T fibroblasts at 20 μM[1].
Autophagy activator-2 (10-80 μM; 24 h) is noncytotoxic to NPC1 fibroblasts[1].
Autophagy activator-2 (80 μM; 24 h) does not inhibit mTOR kinase activity in NPC1I1061T fibroblast[1].
Autophagy activator-2 (80 μM; 24 h) reduces expression of multiple lysosomal hydrolases and increases glycosylated LAMP1 levels in NPC1I1061T fibroblasts[1].
Autophagy activator-2 (80 μM; 24 h) does not reduce unesterified cholesterol accumulation in NPC1 null HeLa cells, demonstrating its activity is dependent on NPC1 expression[1].
Autophagy activator-2 (10, 20 μM; 24 h) increases Endo H-sensitive NPC1 protein levels in fibroblasts, without affecting wild-type NPC1 expression[1].
Autophagy activator-2 (40, 80 μM; 24 h) does not broadly suppress proteasomal or autophagic degradation or alter ATF4 expression in I1061T NPC1 mutant fibroblasts, while elevating the LC3-II/LC3-I ratio and showing no enhanced ER stress[1].

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

Autophagy activator-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: I1061T NPC1 patient-derived fibroblasts
Concentration: 10, 20, 40, 80 μM
Incubation Time: 24 h
Result: Maintained ≥ 80% cell viability at all tested concentrations, showing no cytotoxicity at doses that produce beneficial phenotypic effects.

Western Blot Analysis[1]

Cell Line: I1061T NPC1 patient-derived fibroblasts
Concentration: 80 μM
Incubation Time: 24 h
Result: Did not significantly decrease the formation of phosphorylated p70S6K, indicating no significant inhibition of mTOR kinase activity.\n
Significantly reduced protein expression levels of lysosomal hydrolases including legumain (LGMN), cathepsin Z (CTSZ), cathepsin B (CTSB), and cathepsin D (CTSD).
Increased levels of glycosylated lysosomal-associated membrane protein 1 (LAMP1).

Western Blot Analysis[1]

Cell Line: I1061T NPC1 patient-derived fibroblasts
Concentration: 10, 20 μM
Incubation Time: 24 h
Result: Increased NPC1 protein intensity to ~1.7-fold at 10 μM and ~1.4-fold at 20 μM compared to DMSO treatment.
Increased Endo H-sensitive (ER-retained) I1061T NPC1, with no effect on wild-type NPC1 expression.

Western Blot Analysis[1]

Cell Line: I1061T NPC1 patient-derived fibroblasts
Concentration: 40, 80 μM
Incubation Time: 24 h
Result: Did not cause accumulation of p21, p27, or p62, indicating no broad inhibition of proteasomal or autophagic degradation.
Increased the LC3-II/LC3-I ratio at both 40 and 80 μM, consistent with autophagy modulation.\n
Did not significantly alter ATF4 expression levels compared to DMSO treatment, indicating no exacerbation of ER stress.
Molecular Weight

432.63

Formula

C22H36N6OS
CAS No.
SMILES

CCCCN(CC)CCCNC(C1=C(C)C2=C(N3CCN(C)CC3)N=CN=C2S1)=O
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Storage

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References
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Autophagy activator-2 Related Classifications

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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:

Autophagy activator-21111050-17-9Autophagy activator2Autophagy activator 2AutophagyATF4I1061T NPC1 patient-derived fibroblastseGFP-LC3 HeLa cellsLAMP1niemann-pick type c diseaseautophagyI1061T NPC1unesterified cholesterollysosomal hydrolasemTORInhibitorinhibitorinhibit

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