1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. AES-135

AES-135 

Cat. No.: HY-114483
Handling Instructions

AES-135 is a potent HDAC inhibitor with IC50s of 654 nM, 190 nM, and 636 nM for HDAC3, HDAC6, and HDAC11, respectively. AES-135 has anti-tumor activity.

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

AES-135 Chemical Structure

AES-135 Chemical Structure

CAS No. : 2361659-61-0

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Description

AES-135 is a potent HDAC inhibitor with IC50s of 654 nM, 190 nM, and 636 nM for HDAC3, HDAC6, and HDAC11, respectively. AES-135 has anti-tumor activity[1].

IC50 & Target[1]

HDAC6

190 nM (IC50)

HDAC11

636 nM (IC50)

HDAC3

654 nM (IC50)

In Vitro

AES-135 inhibits cancer cells growth with IC50 values of 2.3 µM, 1.4 µM, 0.27 µM, 0.94 µM, 1.9 µM, 2.72 µM, 2.1 µM, 15.0 µM, 1.6 µM and 19.2 µM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively[1].

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

In Vivo

AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells[1].
NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching Cmax 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h[1].

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

Animal Model: C57Bl/6 mice injected with KPC2 cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 5 days a week; for 1 month
Result: Significantly increased survival of mice.
Molecular Weight

693.66

Formula

C₃₃H₂₉F₆N₃O₅S

CAS No.

2361659-61-0

SMILES

CC(C)(C)C1=CC=C(CN(C(CN(CC2=C(F)C(F)=C(F)C(F)=C2F)S(=O)(C3=CC=C(F)C=C3)=O)=O)C4=CC=C(C(NO)=O)C=C4)C=C1

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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Keywords:

AES-135AES135AES 135HDACHistone deacetylasesHDAC3HDAC6HDAC11anti-tumorpancreaticInhibitorinhibitorinhibit

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AES-135
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HY-114483
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