mTOR/HDAC-IN-1
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent.
For research use only. We do not sell to patients.
- CAS No.: 2815286-02-1
- Formula: C23H23N11O3
- Molecular Weight:501.50
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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 0.49 nM (IC50) |
HDAC1 0.91 nM (IC50) |
HDAC6 86 nM (IC50) |
HDAC8 27 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.16 μM
Compound: 50
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability
Antiproliferative activity against human A549 cells assessed as reduction in cell viability
|
[PMID: 34314844] |
| HCT-116 | IC50 |
3.85 μM
Compound: 50
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
|
[PMID: 34314844] |
| MV4-11 | IC50 |
1.74 μM
Compound: 50
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Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability
|
[PMID: 34314844] |
mTOR/HDAC-IN-1 (Compound 50) (0-10 μM, 72 h) shows remarkable anti-proliferative activity against A549, HCT116, and MV4-11 cells[1].
mTOR/HDAC-IN-1 (0-3 μM, 6 h) simultaneous modulates mTOR signaling and HDAC catalytic activity at cellular level[1].
mTOR/HDAC-IN-1 displays excellent specificity over both HDAC6 and HDAC11 (with IC50 values of 0.91, 86, 27, and >1000 against HDAC1, HDAC6, HDAC8 and HDAC11) [1].
mTOR/HDAC-IN-1 maintains the interaction of MLN0128 with the ATP-binding site in mTOR and binds with the catalytic channel in HDAC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, HCT116, and MV4-11
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Concentration:0-10 μM
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Incubation Time:At 70 h post-compound treatment, to each well was added CCK-8, and the mixture was incubated for additional 2 h.
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Result:Showed anti-proliferative activity with IC50 values of 2.16, 3.85, and 1.74 μM against A549, HCT116, and MV4-11 cells, respectively.
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Cell Line:MV4-11
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Concentration:0.3, 1.0, and 3.0 μM
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Incubation Time:6 h
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Result:Downregulated the levels of Phos-S6 (Ser235/Ser236) and Phos-AKT (Ser473), and elevated the levels of Ac-H3 (K9) and Acα-tubulin (Lys40) in a concentration-dependent manner.
Chemical Information
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CAS No. 2815286-02-1
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Molecular Weight 501.50
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Formula C23H23N11O3
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SMILES
NC1=C(C(C2=CC=C(OC(N)=N3)C3=C2)=N4)C(N4CC(CC5)CCN5C6=NC=C(C(NO)=O)C=N6)=NC=N1
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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)