AR-42

AR-42
Cat. No. : CS-0488 CAS No. : 935881-37-1
M. Wt. : 312.363
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  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: AR-42; HDAC-42;  OSU-HDAC42
Cat. No. : CS-0488
CAS No. : 935881-37-1
Formula: C18H20N2O3
M. Wt. : 312.363
Solubility: 10 mM in DMSO

Activity:

AR-42(HDAC-42) is a HDAC inhibitor with IC50 30 nM. IC50 Value: 30 nM Target: HDAC in vivo: HDAC42 is potent in suppressing the proliferation of U87MG and PC-3 cells, in part, because of its ability to down-regulate Akt signaling. 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. 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. in vitro: 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. AR-42 significantly reduces leukocyte counts, and prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity.

Protocol:

References:

Zhang S, Suvannasankha A, Crean CD, White VL, Chen CS, Farag SS.The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells.Int J Cancer. 2011 Jul 1;129(1):204-13.

Lu YS, Chou CH, Tzen KY, Gao M, Cheng 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.

Shuhong Zhang et al. The novel histone deacetylase inhibitor, AR-42, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells International Journal of Cancer Volume 129, Issue 1, pages 204-213, 1 July 2011

Zimmerman B, Sargeant A, Landes K, Fernandez SA, Chen CS, Lairmore MD.Efficacy of novel histone deacetylase inhibitor, AR42, in a mouse model of, human T-lymphotropic virus type 1 adult T cell lymphoma.Leuk Res. 2011 Nov;35(11):1491-7. Epub 2011 Jul 29.

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.

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