1. PI3K/Akt/mTOR
    Epigenetics
    Cell Cycle/DNA Damage
    Apoptosis
    Autophagy
  2. mTOR
    HDAC
    Apoptosis
    Autophagy
  3. mTOR/HDAC6-IN-1

mTOR/HDAC6-IN-1 

Cat. No.: HY-144449
Handling Instructions

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.

mTOR/HDAC6-IN-1 Chemical Structure

mTOR/HDAC6-IN-1 Chemical Structure

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Description

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)[1].

IC50 & Target[1]

mTOR

133.7 nM (IC50)

HDAC6

56 nM (IC50)

In Vitro

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].

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

Cell Viability Assay

Cell Line: MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1]
Concentration: 0, 20, 40, 60, 80 and 100 μM
Incubation Time: 48 hours
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.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 5, 10, 20 μM
Incubation Time:
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.

Cell Autophagy Assay

Cell Line: MDA-MB-231[1]
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 hours
Result: Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells
Molecular Weight

397.86

Formula

C20H20ClN5O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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mTOR/HDAC6-IN-1
Cat. No.:
HY-144449
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