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AR42

Catalog No. T6392 CAS 935881-37-1

Synonyms: OSU-HDAC42, AR-42, AR 42, HDAC-42

AR42 (OSU-HDAC42) is an HDAC inhibitor (IC50: 30 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

AR42, CAS 935881-37-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 52.00
5 mg	In stock	$ 87.00
10 mg	In stock	$ 167.00
25 mg	In stock	$ 326.00
50 mg	In stock	$ 587.00
100 mg	In stock	$ 793.00
200 mg	In stock	$ 995.00
1 mL * 10 mM (in DMSO)	In stock	$ 96.00

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Purity: 99.46%

Purity: 98.96%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AR42 (OSU-HDAC42) is an HDAC inhibitor (IC50: 30 nM).
Targets&IC50	HDAC:30 nM
In vitro	AR-42 induces p21WAF/CIP1 overexpression and histone hyperacetylation and inhibits the growth of DU-145 cells (IC50 of 0.11 μM) [1]. AR-42 is effective in suppressing the proliferation of PC-3 and U87 mg cells, in part, because of its ability to down-regulate Akt signaling [2]. AR-42 inhibits the growth of PC-3 (IC50: 0.48 μM) and LNCaP (IC50: 0.3 μM) cells. Compared to SAHA, AR-42 has markedly superior apoptogenic potency and causes obviously greater decreases in Bcl-xL, phospho-Akt, and survivin in PC-3 cells [3]. in malignant mast cell lines, AR-42 induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5 [6]. AR-42 effectively inhibits the growth of Raji, JeKo-1, and 697 cells (IC50<0.61 μM). AR-42 also sensitizes CLL cells to TNF-Related Apoptosis-Inducing Ligand (TRAIL), potentially through reduction of c-FLIP [7]. AR-42 also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in HCC cells.
In vivo	The growth of PC-3 tumor xenografts is suppressed by 52% and 67% after treatment with AR-42 (25/50 mg/kg), respectively, whereas SAHA (50 mg/kg) suppresses growth by 31%. In contrast to mice treated with SAHA, intratumoral levels of Bcl-xL and pAkt are markedly reduced in AR-42 treated mice. [3] In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, AR-42 not only decreases the severity of prostatic intraepithelial neoplasia (PIN) and completely prevents its progression to poorly differentiated carcinoma, but also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute (86%) and relative (85%) urogenital tract weights. [5] AR-42 markedly reduces leukocyte counts and prolongs survival in three separate mouse models of B-cell malignancy without toxicity.
Kinase Assay	In vitro HDAC assay:HDAC activity is analyzed by using an HDAC assay kit. This assay is based on the ability of DU-145 nuclear extract, which is rich in HDAC activity, to mediate the deacetylation of the biotinylated [3H]-acetyl histone H4 peptide that is bound to streptavidin agarose beads. The release of [3H]-acetate into the supernatant is measured to calculate the HDAC activity. Sodium butyrate (0.25-1 mM) is used as a positive control.
Cell Research	Concentrations: Dissolved in DMSO,final concentrations ~2.5 μM. Method: DU-145 Cells are exposed to various concentrations of AR-42 for 96 hours.The medium is removed and replaced by 150 μL of 0.5 mg/mL of MTT in RPMI 1640 medium,and the cells are incubated in the CO2 incubator at 37 °C for 2 hours.Supernatants are removed from the wells,and the reduced MTT dye is solubilized with 200 μL/well of DMSO.Absorbance is determined on a plate reader at 570 nm.
Animal Research	Animal Models: Intact male NCr athymic nude mice inoculated s.c.with PC-3 cells. Formulation: Formulated in methylcellulose/Tween 80. Dosages: ~50 mg/kg/day. Administration: p.o.

Synonyms	OSU-HDAC42, AR-42, AR 42, HDAC-42
Molecular Weight	312.36
Formula	C18H20N2O3
CAS No.	935881-37-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 59 mg/mL (188.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 59 mg/mL (188.9 mM)

References and Literature

1. Lu Q, et al. J Med Chem, 2005, 48(17), 5530-5535. 2. Chen CS, et al. J Biol Chem, 2005, 280(46), 38879-38887. 3. Kulp SK, et al. Clin Cancer Res, 2006, 12(17), 5199-5206. 4. Chen CS, et al. Cancer Res, 2007, 67(11), 5318-5327. 5. Sargeant AM, et al. Cancer Res, 2008, 68(10), 31999-42009. 6. Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7(16):22285-94. 7. Su L, Wang S, Yuan T, et al. Anti-oral Squamous Cell Carcinoma Effects of a Potent TAZ Inhibitor AR-42[J]. Journal of Cancer. 2020, 11(2): 364-373. 8. Zhu Y, Yuan T, Zhang Y, et al. AR-42:A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321.

Citations

1. Zhu Y, Yuan T, Zhang Y, et al. AR-42: A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321 2. Zhu Y, Yuan T, Zhang Y, et al. AR-42: A Pan-HDAC Inhibitor with Antitumor and Antiangiogenic Activities in Esophageal Squamous Cell Carcinoma. Drug Design, Development and Therapy. 2019, 13: 4321 3. Su L, Wang S, Yuan T, et al. Anti-oral Squamous Cell Carcinoma Effects of a Potent TAZ Inhibitor AR-42. Journal of Cancer. 2020, 11(2): 364-373.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Pancreatic Cancer Compound Library Cancer Cell Differentiation Compound Library Anti-Breast Cancer Compound Library NF-κB Signaling Compound Library Histone Modification Compound Library

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Keywords

AR42 935881-37-1 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC OSU-HDAC42 HDAC 42 HDAC42 AR-42 AR 42 HDAC-42 inhibitor inhibit

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