mTOR/HDAC6-IN-1
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC).
For research use only. We do not sell to patients.
- CAS No.: 2986747-52-6
- Formula: C20H20ClN5O2
- Molecular Weight:397.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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mTOR 133.7 nM (IC50) |
HDAC6 56 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
8.4 μM
Compound: 10g
|
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs
|
[PMID: 34139324] |
| MDA-MB-436 | IC50 |
10.6 μM
Compound: 10g
|
Antiproliferative activity against human MDA-MB-436 cells measured after 48 hrs
Antiproliferative activity against human MDA-MB-436 cells measured after 48 hrs
|
[PMID: 34139324] |
| MDA-MB-468 | IC50 |
14.3 μM
Compound: 10g
|
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs
|
[PMID: 34139324] |
mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h[1].
mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1]
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Concentration:0, 20, 40, 60, 80 and 100 μM
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Incubation Time:48 hours
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Result:Had a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.
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Cell Line:MDA-MB-231[1]
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Concentration:5, 10, 20 μM
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Incubation Time:
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Result:Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3.
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Cell Line:MDA-MB-231[1]
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Concentration:2.5, 5, 10 μM
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Incubation Time:48 hours
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Result:Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells
Chemical Information
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CAS No. 2986747-52-6
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Molecular Weight 397.86
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Formula C20H20ClN5O2
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SMILES
CN1CCN(CC1)C2=NC(C3=CC=C(C=C3)C(NO)=O)=NC4=CC(Cl)=CC=C42
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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)