DCL1191
DCL1191 is a selective TFEB inhibitor with an IC50 of 60.5 nM and a Kd of 80.5 nM. DCL1191 inhibits Autophagy and disrupts lysosomal function and LAMP1 assembly. DCL1191 increases Temozolomide (HY-17364) sensitivity. DCL1191 can be used for research on glioblastoma.
For research use only. We do not sell to patients.
- Formula: C25H18F4N4O5
- Molecular Weight:530.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
DCL1191 (0-5000 nM; preincubation for 12 hours plus DNA incubation for 2 hours) disrupts WT TFEB-CLEAR DNA binding with an IC50 of 60.5 nM, and this activity is reduced by the TFEB mutations N252A, N252A/R271A, K274A, and I251A[1].
DCL1191 (1.25-10 µM; 12 h) inhibits starvation-induced TFEB target gene expression in HeLa cells; 1.25 µM restores basal expression, while higher concentrations suppress it below baseline[1].
DCL1191 (0.3-5 µM; 2-hour exposure after 16 hours of IL-3 deprivation) exhibits attenuated Tpo-R agonism in BA/F3 cells expressing hTpo-R, with weak STAT5 and STAT3 phosphorylation in the 0.3-5 µM range[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse pro-B BA/F3 cells stably expressing human Tpo-R
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Concentration:0.3, 0.6, 1.2, 2.5, and 5 µM
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Incubation Time:2 h exposure after 16 h IL-3 deprivation
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Result:Produced markedly weaker phosphorylation of both STAT5 and STAT3 across the tested concentration range.
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Cell Line:HeLa cells
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Concentration:1.25, 5, and 10 µM
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Incubation Time:12 h pre-exposure plus 4 h starvation
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Result:Suppressed starvation-induced upregulation of TFEB target genes in a concentration-dependent manner.
At 1.25 µM, restored lysosomal gene transcription to the basal (Normal) level; higher concentrations suppressed expression significantly below baseline.
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Cell Line:HeLa cells
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Concentration:0.6, 1.2, 2.5, 5, and 10 µM
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Incubation Time:12 h pre-incubation plus 2 h starvation with 200 nM Bafilomycin A1
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Result:Relative LC3-II/GAPDH levels were 0.94 at 0.6 µM, 0.96 at 1.2 µM, 0.68 at 2.5 µM, 0.33 at 5 µM, and 0.19 at 10 µM.
LC3-II inhibition was 69% at 5 µM and 80% at 10 µM.
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Cell Line:U87 glioblastoma cells
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Concentration:5 and 10 µM
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Incubation Time:12 h
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Result:Abrogated LC3 puncta formation, producing a diffuse cytosolic and nuclear distribution pattern typical of non-autophagic states.
Disrupted LAMP1 assembly, indicating impaired lysosomal function.
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Cell Line:U87 glioblastoma cells
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Concentration:0.625, 1.25, 5, 10, and 20 µM (DCL1191); 0-500 µM (TMZ)
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Incubation Time:72 h
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Result:In combination with TMZ, produced a robust synergistic effect with an HSA synergy score of 17.51.
Parmacokinetics
Chemical Information
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Molecular Weight 530.43
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Formula C25H18F4N4O5
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SMILES
COC1=CC(C2=C(O)C(N/N=C3C(N(C4=CC=C(C(F)(F)F)C=C4)N=C\3C)=O)=CC(F)=C2)=CC(C(O)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DCL1191 Related Classifications
HY-190943 Related Classifications
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