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AR-42 (HDAC-42, NSC-736012, OSU-42)

Alias: HDAC-42; AR42; AR 42; AR-42; (S)-HDAC-42; AR-42; NSC-736012; OSU-42; OSU 42; OSU42; OSU-HDAC-42; OSU HDAC-42; OSU HDAC 42; OSUHDAC-42
Cat No.:V0283 Purity: ≥98%
COA Product Data Instructions for use SDS
AR-42 (HDAC-42, NSC-736012, OSU-42 etc.) is a novel and potent histone deacetylase (HDAC) inhibitor with potential antitumor activity. At 30 nM, its IC50 inhibits HDAC.
AR-42 (HDAC-42, NSC-736012, OSU-42) Chemical Structure CAS No.: 935881-37-1
Product category: HDAC
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

COA
MSDS
NMR
Instructions
Product Description

AR-42 (HDAC-42, NSC-736012, OSU-42 etc.) is a novel and potent histone deacetylase (HDAC) inhibitor with potential antitumor activity. At 30 nM, its IC50 inhibits HDAC. It exhibits strong in vivo antitumor efficacy against a variety of tumor types, including hepatic and prostate cancers, as well as strong anti-proliferative activity against different cancer cell lines.

Biological Activity I Assay Protocols (From Reference)
Targets
HDAC ( IC50 = 16 nM )
ln Vitro

In vitro activity: AR-42 treatment causes p21WAF/CIP1 overexpression and histone hyperacetylation, and it inhibits DU-145 cell growth with an IC50 of 0.11 μM. [1] HDAC42's capacity to inhibit Akt signaling contributes to its effectiveness in inhibiting the growth of PC-3 and U87MG cells. The growth of PC-3 and LNCaP cells is inhibited by AR-42, with IC50 values of 0.48 μM and 0.3 μM, respectively. In PC-3 cells, AR-42 significantly reduces phospho-Akt, Bcl-xL, and survivin and has a significantly higher apoptogenic potency than SAHA. [3] In malignant mast cell lines, treatment with AR-42 causes growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. Treatment with AR-42 results in down-regulation of Kit through HSP70 up-regulation, disassociation between Kit and heat shock protein 90 (HSP90), and inhibition of Kit transcription. The expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5 is downregulated in response to AR-42 treatment. [6] AR-42 exhibits potent growth inhibition of Raji, 697, and JeKo-1 cells, with an IC50 of less than 0.61 μM. Additionally, AR-42 increases the susceptibility of CLL cells to TNF-Related Apoptosis Inducing Ligand (TRAIL), possibly by lowering c-FLIP. [7] By downregulating Akt/mTOR signaling and creating ER stress in hepatocellular carcinoma (HCC) cells, AR-42 treatment also promotes autophagy. [8]
ln Vivo
Treatment with 25 mg/kg and 50 mg/kg of AR-42 suppresses the growth of PC-3 tumor xenografts by 52% and 67%, respectively, while treatment with 50 mg/kg of SAHA suppresses growth by 31%. Mice treated with AR-42 exhibit significantly lower intratumoral levels of phospho-Akt and Bcl-xL compared to those treated with SAHA.[3] AR-42 administration not only completely prevents the progression of prostatic intraepithelial neoplasia (PIN) to poorly differentiated carcinoma in the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, but it also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute and relative urogenital tract weights by 86% and 85%, respectively.[5] In three different mouse models of B-cell cancer, AR-42 dramatically lowers leukocyte counts and extends survival without showing any signs of toxicity.[7]
Enzyme Assay
Using an HDAC assay kit, HDAC activity is measured. This assay is based on the observation that the biotinylated [3H]-acetyl histone H4 peptide bound to streptavidin agarose beads can be deacetylated through the action of DU-145 nuclear extract, which is high in HDAC activity. The HDAC activity is determined by measuring the amount of [3H]-acetate released into the supernatant. A positive control is employed, namely sodium butyrate (0.25-1 mM).
Cell Assay
For ninety-six hours, cells are exposed to varying concentrations of AR-42. After removing the medium, 150 μL of 0.5 mg/mL MTT in RPMI 1640 medium is added, and the cells are incubated for two hours at 37 °C in a CO2 incubator. After removing the supernatants from the wells, 200 μL of DMSO per well is used to solubilize the reduced MTT dye. At 570 nm, absorbance is measured on a plate reader.
Animal Protocol
Dissolved in methylcellulose/Tween 80; 50 mg/kg/day; Oral gavage
Intact male NCr athymic nude mice inoculated s.c. with PC-3 cells
References

[1]. J Med Chem . 2005 Aug 25;48(17):5530-5.

[2]. J Biol Chem . 2005 Nov 18;280(46):38879-87.

[3]. Clin Cancer Res . 2006 Sep 1;12(17):5199-206.

[4].Cancer Res . 2007 Jun 1;67(11):5318-27.

[5]. Cancer Res . 2008 May 15;68(10):3999-4009.

[6]. Blood . 2010 May 27;115(21):4217-25.

[7]. PLoS One . 2010 Jun 3;5(6):e10941.

[8]. Autophagy . 2010 Nov;6(8):1057-65.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H20N2O3
Molecular Weight
312.36
Exact Mass
312.15
Elemental Analysis
C, 69.21; H, 6.45; N, 8.97; O, 15.37
CAS #
935881-37-1
Related CAS #
935881-37-1
Appearance
Solid powder
SMILES
CC(C)[C@@H](C1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)C(=O)NO
InChi Key
LAMIXXKAWNLXOC-INIZCTEOSA-N
InChi Code
InChI=1S/C18H20N2O3/c1-12(2)16(13-6-4-3-5-7-13)18(22)19-15-10-8-14(9-11-15)17(21)20-23/h3-12,16,23H,1-2H3,(H,19,22)(H,20,21)/t16-/m0/s1
Chemical Name
N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide
Synonyms
HDAC-42; AR42; AR 42; AR-42; (S)-HDAC-42; AR-42; NSC-736012; OSU-42; OSU 42; OSU42; OSU-HDAC-42; OSU HDAC-42; OSU HDAC 42; OSUHDAC-42
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 10~63 mg/mL (32.0~201.7 mM)
Water: <1 mg/mL
Ethanol: 50~63 mg/mL (160.1~201.7 mM)
Solubility (In Vivo)
0.5% methylcellulose+0.2% Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.

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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02569320 Completed Drug: Dexamethasone
Drug: HDAC Inhibitor AR-42		 Recurrent Plasma Cell Myeloma Ohio State University
Comprehensive Cancer Center		 May 20, 2016 Phase 1
NCT01798901 Completed Drug: HDAC inhibitor AR-42
Drug: decitabine		 Adult Acute Myeloid Leukemia
With Inv(16)(p13;q22)
Adult Acute Myeloid Leukemia
With t(15;17)(q22;q12)		 Alison Walker September 17, 2013 Phase 1
NCT02282917 Completed Drug: AR-42 Vestibular Schwannoma
Meningioma		 Massachusetts Eye and Ear
Infirmary		 December 2015 Early Phase 1
NCT02795819 Terminated Drug: AR-42
Drug: Pazopanib		 Renal Cell Carcinoma
Soft Tissue Sarcoma		 Virginia Commonwealth
University		 July 8, 2016 Phase 1
Biological Data

  • AR-42

    AR-42

  • AR-42
    OSU-HDAC42 suppressed the development of prostate lesions in 10-wk-old TRAMP mice.Cancer Res.2008 May 15;68(10):3999-4009.



    AR-42
    OSU-HDAC42 prevented the progression of prostate lesions to poorly differentiated carcinoma in 24-wk-old TRAMP mice.Cancer Res.2008 May 15;68(10):3999-4009.
  • AR-42
    Characterization of OSU-HDAC42–associated testicular degeneration.Cancer Res.2008 May 15;68(10):3999-4009.
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