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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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mTOR 0.49 nM (IC50) |
HDAC1 0.91 nM (IC50) |
HDAC6 86 nM (IC50) |
HDAC8 27 nM (IC50) |
Cellular Effect
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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
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[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
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[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
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[PMID: 34314844] |
In Vitro
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. Further protocols information, click here.
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
mTOR/HDAC-IN-1 Related Classifications
HY-141701 Related Classifications
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