AR42

SKU: orb1300808

Description

AR42

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 935881-37-1
• MW: 312.36
• Purity: 98.46%
• Formula: C₁₈H₂₀N₂O₃
• SMILES: CC(C)[C@H](C(=O)Nc1ccc(cc1)C(=O)NO)c1ccccc1
• Target: Autophagy,HDAC,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:59 mg/mL (188.88 mM);DMSO:59 mg/mL (188.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.2 mM)

Bioactivity

• Target IC50:
  HDAC:30 nM
• 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. 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. AR-42 markedly reduces leukocyte counts and prolongs survival in three separate mouse models of B-cell malignancy without toxicity.
• In Vitro:
  AR-42 induces p21WAF/CIP1 overexpression and histone hyperacetylation and inhibits the growth of DU-145 cells (IC50 of 0.11 μM) . 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 . 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 . 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 . 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 . AR-42 also induces autophagy through downregulation of Akt/mTOR signaling and inducing ER stress in HCC cells.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AR 42, AR42, AR-42, OSU-HDAC42, HDAC, HDAC 42, HDAC42, HDAC-42

Compound Identifiers

PubChem CID

6918848