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AR-42 (HDAC-42)

AR-42 (HDAC-42, OSU-HDAC42) is a pan-HDAC inhibitor with IC50 30 nM.

Catalog No.S2244

: Tel: +1-832-582-8158[email protected]

AR-42 (HDAC-42) Chemical Structure
Molecular Weight: 312.36

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

AR-42 (HDAC-42) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Epigenetics Compound Library (96-well) Inhibitor Library (96-well)

Product Information

Combination Therapy

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Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1053	Entinostat (MS-275, SNDX-275)	<1 mg/mL	75 mg/mL	<1 mg/mL
S1047	Vorinostat (SAHA)	<1 mg/mL	53 mg/mL	3 mg/mL
S1030	Panobinostat (LBH589)	<1 mg/mL	70 mg/mL	<1 mg/mL
S3020	Romidepsin (FK228 ,depsipeptide)	<1 mg/mL	10 mg/mL	<1 mg/mL
S1045	Trichostatin A (TSA)	<1 mg/mL	23 mg/mL	<1 mg/mL
S1122	Mocetinostat (MGCD0103)	<1 mg/mL	13 mg/mL	<1 mg/mL
S2627	Tubastatin A HCl	<1 mg/mL	74 mg/mL	<1 mg/mL
S1085	Belinostat (PXD101)	<1 mg/mL	64 mg/mL	<1 mg/mL
S2170	ITF2357 (Givinostat)	<1 mg/mL	95 mg/mL	3 mg/mL
S1095	LAQ824 (NVP-LAQ824, Dacinostat)	<1 mg/mL	76 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S1515	SB939 (Pracinostat)	<1 mg/mL	72 mg/mL	27 mg/mL
S2012	PCI-34051	<1 mg/mL	59 mg/mL	<1 mg/mL
S1422	Droxinostat	<1 mg/mL	49 mg/mL	49 mg/mL
S1484	MC1568	<1 mg/mL	13 mg/mL	<1 mg/mL
S1090	PCI-24781	<1 mg/mL	80 mg/mL	<1 mg/mL
S1096	JNJ-26481585	<1 mg/mL	79 mg/mL	<1 mg/mL
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S2818	CI994 (Tacedinaline)	<1 mg/mL	≥54 mg/mL	<1 mg/mL
S2244	AR-42 (HDAC-42)	<1 mg/mL	63 mg/mL	63 mg/mL
S2779	M344	<1 mg/mL	62 mg/mL	4 mg/mL
S2759	PI3K/HDAC InhibitorⅠ	<1 mg/mL	102 mg/mL	<1 mg/mL
S8001	Rocilinostat (ACY-1215)	<1 mg/mL	87 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	AR-42 (HDAC-42, OSU-HDAC42) is a pan-HDAC inhibitor with IC50 30 nM.
Targets	HDAC
IC50	30 nM ^[1]
In vitro	AR-42 treatment induces histone hyperacetylation and p21^WAF/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]
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]
Clinical Trials	A Phase I study of AR-42 in treating patients with advanced or relapsed multiple myeloma, chronic lymphocytic leukemia, or lymphoma is currently ongoing.
Features	More potent than SAHA.

Protocol(Only for Reference)

Kinase Assay:
^[1]

In vitro HDAC assay	HDAC activity is analyzed by using a 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.

In vitro HDAC assay

HDAC activity is analyzed by using a 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 Assay:
^[1]

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.

Animal Study:
^[3]

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

References

Chemical Information

Download AR-42 (HDAC-42) SDF

Molecular Weight (MW)	312.36
Formula	C₁₈H₂₀N₂O₃
CAS No.	935881-37-1
Synonyms	OSU-HDAC42

Solubility (25°C) DMSO 63 mg/mL Water <1 mg/mL Ethanol 63 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	(S)-N-hydroxy-4-(3-methyl-2-phenylbutanamido)benzamide

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Trichostatin A (TSA)

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Entinostat (MS-275, SNDX-275)

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Belinostat (PXD101)

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PCI-24781

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JNJ-26481585

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Mocetinostat (MGCD0103)

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CUDC-101

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Epigenetics Pathway Products

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AR-42 (HDAC-42) + Bleomycin-sulfate	Pretreatment of DU-145 cells with 0.25 μM AR-42 augments the effect of Bleomycin, Doxorubicin, and VP-16, but not Fluorouracil, on clonogenic inhibition, by targeting Ku70 acetylation. ^[4]
AR-42 (HDAC-42) + Adriamycin	Pretreatment of DU-145 cells with 0.25 μM AR-42 augments the effect of Bleomycin, Doxorubicin, and VP-16, but not Fluorouracil, on clonogenic inhibition, by targeting Ku70 acetylation. ^[4]
AR-42 (HDAC-42) + Etopophos	Pretreatment of DU-145 cells with 0.25 μM AR-42 augments the effect of Bleomycin, Doxorubicin, and VP-16, but not Fluorouracil, on clonogenic inhibition, by targeting Ku70 acetylation. ^[4]

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AR-42 (HDAC-42)