1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. ACY-738

ACY-738 

Cat. No.: HY-19327 Purity: 99.94%
Handling Instructions

ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.

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

ACY-738 Chemical Structure

ACY-738 Chemical Structure

CAS No. : 1375465-91-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 588 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.

IC50 & Target[1]

HDAC6

1.7 nM (IC50)

HDAC1

94 nM (IC50)

HDAC2

128 nM (IC50)

HDAC3

218 nM (IC50)

In Vitro

ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells[1]. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228[3].

In Vivo

ACY-738 (5 mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50 mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment[1]. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels[2].

Molecular Weight

270.29

Formula

C₁₄H₁₄N₄O₂

CAS No.

1375465-91-0

SMILES

O=C(NO)C(C=N1)=CN=C1NC2(CC2)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (118.39 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6997 mL 18.4986 mL 36.9973 mL
5 mM 0.7399 mL 3.6997 mL 7.3995 mL
10 mM 0.3700 mL 1.8499 mL 3.6997 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice are injected i.p. 5 days/week with the vehicle control (DMSO), ACY-738 treatment at 5 mg/kg (low-dose), or ACY-738 treatment at 20 mg/kg (high-dose) beginning at 22-weeks-of-age until euthanasia at 38 weeks-of-age. The total volume injected is 80 μL. Proteinuria and weight are measured every 2 weeks and blood is collected every four weeks for sera analysis. Proteinuria is measured by a standard semi-quantitative test using Siemens Uristix dipsticks. Results are quantified and scored as follows: dipstick reading of 0 mg/dL = 0, trace = 1, 30-100 mg/dL = 2, 100-300 mg/dL = 3, 300-2000 mg/dL = 4, and 2000 + mg/dL = 5[2].

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

References
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ACY-738
Cat. No.:
HY-19327
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