AR-42 (OSU-HDAC42)

Catalog #

27603-1

$195 *

Size: 5 mg

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Description

AR-42 (also known as OSU-HDAC42), a derivative of hydroxamate-tethered phenylbutyrate is a broad-spectrum deacetylase inhibitor of both histone and non-histone proteins. AR-42 treatment induces histone hyperacetylation and p21WAF/CIP1 overexpression, inhibits gp130/Stat3 pathway and induces apoptosis and cell cycle arrest in multiple myeloma cells.

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Synonyms

OSU-HDAC42; N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide

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Product Data Gallery

Product Info

Storage and Usage

Citations

Purity

≥99% by HPLC

Target(s)

HDAC

Formula

C₁₈H₂₀N₂O₃

312.4 Da

Solubility

Soluble in DMSO

Biological Activity

AR-42 is a pan-HDAC inhibitor with IC50 of 16-30 nM. It has demonstrated greater potency and activity in solid tumors and hematological malignancies (including chronic lymphocyte leukemia, or CLL, B-cell lymphoma, prostate and ovarian cancers) when compared to vorinostat (SAHA), the first of two marketed compound in the class.

CAS Registry #

935881-37-1

Background

AR-42 induces histone H3 acetylation, α-tubulin acetylation and p21 up-regulation, which have been considered as the hallmark indicators of HDAC inhibition. AR-42 has been found to modulate several apoptosis inhibitors as well as cell survival regulator, including Akt, Bcl-xL, Bax, Ku70 and surviving, and exert potent antitumor activity against multiple tumor types, such as human prostate and hepatic cancers, at least partially through PI3K/Akt pathway inhibition. AR-42 has been designated an orphan drug by the FDA for the treatment of meningioma and schwannoma of the central nervous system. Meningioma and schwannoma are rare, benign tumors that can present in different locations within the brain and the spinal cord and may cause substantial morbidity.

References

1. Burns, S.S., et al. Cancer Res. 2013 Jan 15;73(2):792-803.
2. Zhang, S., et al. Int J Cancer. 2011 Jul 1;129(1):204-13.
3. Lucas, D.M., et al. PLoS One. 2010 Jun 3;5(6):e10941

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AR-42 (OSU-HDAC42)

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