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Formula | C18H20N2O3 |
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Molecular Weight | 312.36 | CAS No. | 935881-37-1 | ||||
Solubility (25°C)* | In vitro | DMSO | 62 mg/mL (198.48 mM) | ||||
Ethanol | 62 mg/mL (198.48 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1. | ||
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Targets |
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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] | ||
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] | ||
Features | Greater potency relative to SAHA. |
Kinase Assay: |
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Data from [Data independently produced by Sci Transl Med, 2014, 6(256), 256ra135]
Data from [Data independently produced by Leuk Res, 2014, 8(11), 1320-6]
, , J Cell Physiol, 2017, 233(1):559-571
Data from [Data independently produced by , , Oncotarget, 2016, 7(16):22285-94.]
Orthogonal proteogenomic analysis identifies the druggable PA2G4-MYC axis in 3q26 AML [ Nat Commun, 2024, 15(1):4739] | PubMed: 38834613 |
Fermented Wheat Germ Protein with Histone Deacetylase Inhibitor AR42 Demonstrates Enhanced Cytotoxicity against Lymphoma Cells In Vitro and In Vivo [ Int J Mol Sci, 2024, 25(14)7866] | PubMed: 39063110 |
Peripheral blood DNA methylation and neuroanatomical responses to HDACi treatment that rescues neurological deficits in a Kabuki syndrome mouse model [ Clin Epigenetics, 2023, 10.1186/s13148-023-01582-x] | PubMed: 37884963 |
Peripheral blood DNA methylation and neuroanatomical responses to HDACi treatment that rescues neurological deficits in a Kabuki syndrome mouse model [ Clin Epigenetics, 2023, 15(1):172] | PubMed: 37884963 |
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] | PubMed: 36230806 |
The histone H3-lysine 4-methyltransferase Mll4 regulates the development of growth hormone-releasing hormone-producing neurons in the mouse hypothalamus [ Nat Commun, 2021, 12(1):256] | PubMed: 33431871 |
KMT2D Deficiency Impairs Super-Enhancers to Confer a Glycolytic Vulnerability in Lung Cancer. [ Cancer Cell, 2020, 13;37(4):599-617 e7] | PubMed: 32243837 |
A library of aminoglycoside-derived lipopolymer nanoparticles for delivery of small molecules and nucleic acids [ J Mater Chem B, 2020, 8(37):8558-8572] | PubMed: 32830211 |
Identification of Combinations of Protein Kinase C Activators and Histone Deacetylase Inhibitors That Potently Reactivate Latent HIV [ Viruses, 2020, 3;12(6):E609] | PubMed: 32503121 |
Heme oxygenase-1 reduces the sensitivity to imatinib through nonselective activation of histone deacetylases in chronic myeloid leukemia [Wei D, et al. J Cell Physiol, 2019, 234(4):5252-5263] | PubMed: 30256411 |
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