1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. AES-350

AES-350 

Cat. No.: HY-138831 Purity: 98.02%
Handling Instructions

AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC-3, -8, and -11 in an enzymatic activity assay with IC50 values of 0.187 μM, 0.245 μM, and >1μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

For research use only. We do not sell to patients.

AES-350 Chemical Structure

AES-350 Chemical Structure

CAS No. : 847249-57-4

Size Price Stock Quantity
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC-3, -8, and -11 in an enzymatic activity assay with IC50 values of 0.187 μM, 0.245 μM, and >1μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research[1].

IC50 & Target[1]

HDAC6

24.4 nM (IC50)

HDAC3

187 nM (IC50)

HDAC11

245 nM (IC50)

In Vitro

In contrast, AES-350 has submicromolar activity (IC50=0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC50=0.31±0.061 μM). AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC50>30 μM in noncancerous MRC-9 cells). AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC50=0.73 ± 0.12 μM)[1].
AES-350 (0.25-4 μM; 18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner. The late apoptosis ratios are 8.74%, 11.7%,16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM[1].
An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350. Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC50=0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC[1].

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

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.25 μM; 0.5 μM; 1.00 μM; 2.00 μM; 4.00 μM
Incubation Time: 18 hours
Result: Revealed a clear dosedependent increase in the percentage of cells entering late-stage apoptosis, similar to SAHA.
In Vivo

AES-350 (oral gavage; 20 mg/kg; single dose) exhibits a relative good pharmacokinetic (PK) properties in CD-1 mice. The single dose oral bioavailability (F%) of 51 is 19.8%. In comparison, the reported F% for SAHA in mice is significantly lower (8%)[1].

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

Molecular Weight

312.36

Formula

C₁₈H₂₀N₂O₃

CAS No.
SMILES

O=C(NO)C1=CC=C(NC(C2=CC=C(C(C)(C)C)C=C2)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (320.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2014 mL 16.0072 mL 32.0143 mL
5 mM 0.6403 mL 3.2014 mL 6.4029 mL
10 mM 0.3201 mL 1.6007 mL 3.2014 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AES-350AES350AES 350HDACHistone deacetylasesacute myeloid leukemiaAMLMV4-11Inhibitorinhibitorinhibit

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AES-350
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