AR-42 (Synonyms: HDAC-42; OSU-HDAC42)

Name: AR-42
Brand: MedChemExpress
SKU: HY-13265
Rating: 4.5 (4 reviews)

Cat. No.: HY-13265 Purity: 98.69%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC₅₀=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines.

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

AR-42 Chemical Structure

CAS No. : 935881-37-1

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 105	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 105	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

2 Publications Citing Use of MCE AR-42

: AR-42 purchased from MedChemExpress. Usage Cited in: J Cell Physiol . 2019 Dec;234(12):22411-22423. [Abstract]; Western blot shows that AR-42 induces cell apoptosis by inducing caspase3/9 and PARP cleavage.

: AR-42 purchased from MedChemExpress. Usage Cited in: J Cell Physiol . 2019 Dec;234(12):22411-22423. [Abstract]; Western blot shows dose-dependent increases in the levels of acetylated histone H3 after AR-42 treatment for 48 hr.

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Biological Activity
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Description

IC₅₀ & Target

IC50: 16 nM (HDAC)^[2]

In Vitro

AR-42 (0.125-1 μM; 24 hours) inhibits cell proliferation in a dose-dependent manner, and the median IC₅₀s for P815, C2, and BR cells are 0.65, 0.30, and 0.23 μM, respectively^[3].
AR-42 (0.5 μM; 24 hours) induces cell-cycle arrest at G1 in the P815 cells and at G1/G2 in the C2 cells^[3].
AR-42 (0.13-1 μM; 24 hours) causes a dose-dependent induction of apoptosis P815, C2, BR cells^[3].
AR-42 (0.5-3 μM; 24 hours) induces hyperacetylation of histones H3 and H4 and α-tubulin^[3].

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

Cell Proliferation Assay^[3]

Cell Line:	Mouse (P815) and canine (C2 and BR) malignant mast cells
Concentration:	0.0625, 0.125, 0.25, 0.5, 1 μM
Incubation Time:	24 hours
Result:	Inhibited cell proliferation in a dose-dependent manner, and the median IC₅₀s for P815, C2, and BR cells were 0.65, 0.30, and 0.23 μM, respectively.

Cell Cycle Analysis^[3]

Cell Line:	P815,C2 cells
Concentration:	0.5 μM
Incubation Time:	24 hours
Result:	Induced cell-cycle arrest at G1 in the P815 cells and at G1/G2 in the C2 cells.

Apoptosis Analysis^[3]

Cell Line:	P815, C2, BR cells
Concentration:	0.13, 0.25, 0.5, 1 μM
Incubation Time:	24 hours
Result:	Caused a dose-dependent induction of apoptosis.

Western Blot Analysis^[3]

Cell Line:	P815, C2, BR cell lines
Concentration:	0.5, 1, 3 μM
Incubation Time:	24 hours
Result:	A dose-dependent hyperacetylation of histone H3, histone H4, and α-tubulin.

In Vivo

AR-42 (10 mg/kg; tail vein injection; twice a week for three weeks) significantly inhibites tumor growth^[4].

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

Animal Model:	Nude mice (HepG2 cell tumor xenograft model) ^[4]
Dosage:	10 mg/kg
Administration:	Tail vein injection; twice a week for three weeks
Result:	Significantly inhibited tumor growth.

Clinical Trial

Molecular Weight

312.36

Formula

C₁₈H₂₀N₂O₃

CAS No.

935881-37-1

Appearance

Solid

Color

White to light brown

SMILES

CC([C@@H](C1=CC=CC=C1)C(NC2=CC=C(C=C2)C(NO)=O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

Ethanol : 50 mg/mL (160.07 mM; Need ultrasonic)

DMSO : 10 mg/mL (32.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (16.01 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (16.01 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 5 mg/mL (16.01 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (3.20 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.20 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (3.20 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.69%

Select Batch:

Data Sheet (279 KB) SDS (0 KB)

COA (248 KB) RP-HPLC (247 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Lu YS, Chou CH, Tzen KY, Gao M, ChLu YS, et al. Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma. Int J Radiat Oncol Biol Phys. 2012 Jun 1;83(2):e181-9.eng AL, Kulp SK, Cheng JC.Radiosensitizing effect of a phenylbutyrate-derived histone deacetylase inhibitor in hepatocellular carcinoma.Int J Radiat Oncol Biol Phys. 2012 Jun 1;83(2):e181-9. Epub 2012 Feb 28. [Content Brief]

[2]. Lu Q, et al. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5. [Content Brief]

[3]. Lin TY, et al. AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Blood. 2010 May 27;115(21):4217-25. [Content Brief]

[4]. Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7(16):22285-94. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	3.2014 mL	16.0072 mL	32.0143 mL	80.0359 mL
	5 mM	0.6403 mL	3.2014 mL	6.4029 mL	16.0072 mL
	10 mM	0.3201 mL	1.6007 mL	3.2014 mL	8.0036 mL
	15 mM	0.2134 mL	1.0671 mL	2.1343 mL	5.3357 mL
	20 mM	0.1601 mL	0.8004 mL	1.6007 mL	4.0018 mL
	25 mM	0.1281 mL	0.6403 mL	1.2806 mL	3.2014 mL
	30 mM	0.1067 mL	0.5336 mL	1.0671 mL	2.6679 mL
Ethanol	40 mM	0.0800 mL	0.4002 mL	0.8004 mL	2.0009 mL
	50 mM	0.0640 mL	0.3201 mL	0.6403 mL	1.6007 mL
	60 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3339 mL
	80 mM	0.0400 mL	0.2001 mL	0.4002 mL	1.0004 mL
	100 mM	0.0320 mL	0.1601 mL	0.3201 mL	0.8004 mL

AR-42 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AR-42935881-37-1HDAC-42 OSU-HDAC42AR42AR 42HDAC42HDAC 42HDACAutophagyApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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AR-42 (Synonyms: HDAC-42; OSU-HDAC42)

Customer Review

AR-42 Related Antibodies

2 Publications Citing Use of MCE AR-42

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•Related Small Molecules:

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View All HDAC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AR-42 Related Antibodies

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Complete Stock Solution Preparation Table

AR-42 Related Classifications

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