AR-42

Catalog No.S2244 Synonyms: HDAC-42

AR-42 Chemical Structure

Molecular Weight(MW): 312.36

AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 70 In stock
USD 150 In stock
USD 270 In stock
USD 970 In stock
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Cited by 13 Publications

6 Customer Reviews

  • One- to 2-month-old mice of both genotypes showed an increase in H3K4me3 (n = 5 to 6 per group) associated with a dose-dependent increase in neurogenesis in Kmt2d+/βGeo mice (monitored by normalized DCX expression) (n = 4 to 6 per group) upon treatment with the HDACi AR-42. There was no difference in either H3K4me3 or neurogenesis between Kmt2d+/βGeo and Kmt2d+/+ animals at a dose of 10 mg/kg per day.

    Sci Transl Med 2014 6(256), 256ra135. AR-42 purchased from Selleck.

  • Colony formation assay showed significant inhibition following HB22.7 and AR42 treatment. Raji cells in semi-solid medium were treated with AR42 (0.25 uM), HB22.7 (0.4 ug/ml), or both. AR42 significantly inhibited anchorage-independent growth but the combination treatment further inhibited colony formation, *p<0.001.

    Leuk Res 2014 8(11), 1320-6. AR-42 purchased from Selleck.

  • The serum-deprived control or Runx2 knockdown cells were treated with AR-42 for 6 hr at indicated concentrations. The LC3B-II, acetylated-α-tubulin, and β-Actin levels were evaluated by western blotting. The β-Actin normalized LC3B-II expression levels are indicated below each lane.

    J Cell Physiol, 2017, 233(1):559-571. AR-42 purchased from Selleck.

  • Cells were treated with AR-42 and quantified via CCK-8 assay (A).

    Oncotarget, 2016, 7(16):22285-94.. AR-42 purchased from Selleck.

  • HDAC5-overexpressing HepG2 cells were treated with AR-42 and subjected to western blot (A)

    Oncotarget, 2016, 7(16):22285-94. AR-42 purchased from Selleck.

  • The serum-deprived control or Runx2 knockdown cells were treated with AR-42 for 6 hr at indicated concentrations. The LC3B-II, acetylated-α-tubulin, and β-Actin levels were evaluated by western blotting. The β-Actin normalized LC3B-II expression levels are indicated below each lane.

    J Cell Physiol, 2018, 233(1):559-571. AR-42 purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
Features Greater potency relative to SAHA.
Targets
HDAC [1]
(Cell-free assay)
30 nM
In vitro

AR-42 treatment induces histone hyperacetylation and p21WAF/CIP1 overexpression, and inhibits the growth of DU-145 cells with IC50 of 0.11 μM. [1] HDAC42 is potent in suppressing the proliferation of U87MG and PC-3 cells, in part, because of its ability to down-regulate Akt signaling. [2] AR-42 inhibits the growth of PC-3 and LNCaP cells with IC50 of 0.48 μM and 0.3 μM, respectively. Compared to SAHA, AR-42 exhibits distinctly superior apoptogenic potency, and causes markedly greater decreases in phospho-Akt, Bcl-xL, and survivin in PC-3 cells. [3] AR-42 treatment induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7 in malignant mast cell lines. AR-42 treatment induces down-regulation of Kit via inhibition of Kit transcription, disassociation between Kit and heat shock protein 90 (HSP90), and up-regulation of HSP70. AR-42 treatment down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5. [6] AR-42 potently inhibits the growth of JeKo-1, Raji, and 697 cells with IC50 of <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 treatment also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in hepatocellular carcinoma (HCC) cells. [8]

Assay
Methods Test Index PMID
Western blot
gp130 / p-STAT3 / STAT3 / p-AKT / AKT / p-MEK / MEK ; 

PubMed: 20824695     


U266 cells were treated for 24 hr with or without AR-42 and analyzed for the indicated protein by immunoblotting.

Cyclin D1 / p21 / p16 / Cyclin A / Cyclin B1 ; 

PubMed: 20824695     


AR-42 induces expression of p16 and p21 and reduces expression of cyclin D1. U266 cells were treated with 0.05% DMSO or AR-42 at the shown concentrations for 24 hr. Lysates were then prepared immediately and analyzed by Western blot for cyclin D1, p21, p16, cyclin A and cyclin B.

Act-H3 / Act-H3 / Act-tubulin ; 

PubMed: 20233974     


AR-42 treatment induces acetylation of histones and α-tubulin in malignant mast cells. P815, C2, and BR cell lines were treated with the indicated concentrations of AR-42 or 1μM 17-AAG and canine BMCMCs were treated with 1μM AR-42 or 17-AAG for 24 hours. Effects on the acetylation status of histones H3 and H4 and α-tubulin were determined by Western blotting.

p-Kit / Kit ; 

PubMed: 20233974     


P815, C2, and BR cells and canine BMCMCs were treated with either AR-42 or 17-AAG (1μM AR-42 and 17-AAG for BMCMCs) at the indicated concentrations for 24 hours. Effects on the expression of phosphorylated Kit and total Kit were determined by Western blot analysis. The top band represents the mature form and the bottom band the immature form of Kit. 

Notch1 / NICD / Nestin / Zeb-1 / BMI-1 ; 

PubMed: 26625202     


The expression levels of acetyl-histone H3 (Ac-H3), Notch1, NICD, and/or the downstream stemness markers nestin, Zeb-1, and BMI-1 in MDA-MB-231 after 72 h of treatment.

20824695 20233974 26625202
Growth inhibition assay
Cell viability; 

PubMed: 26993777     


Cells were treated with AR-42 and quantified via CCK-8 assay.

26993777
In vivo The growth of PC-3 tumor xenografts is suppressed by 52% and 67% after treatment with AR-42 at 25 mg/kg and 50 mg/kg, respectively, whereas SAHA at 50 mg/kg suppresses growth by 31%. In contrast to mice treated with SAHA, intratumoral levels of phospho-Akt and Bcl-xL are markedly reduced in AR-42 treated mice. [3] In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, administration of 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 and relative urogenital tract weights by 86% and 85%, respectively. [5] AR-42 significantly reduces leukocyte counts, and prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity. [7]

Protocol

Kinase Assay:

[1]

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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:

[1]

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  • Cell lines: DU-145
  • Concentrations: Dissolved in DMSO, final concentrations ~2.5 μM
  • Incubation Time: 96 hours
  • Method:

    Cells are exposed to varous 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.


    (Only for Reference)
Animal Research:

[3]

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  • 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: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (201.69 mM)
Ethanol 63 mg/mL (201.69 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 312.36
Formula

C18H20N2O3

CAS No. 935881-37-1
Storage powder
in solvent
Synonyms HDAC-42

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID