| Bioactivity | AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines[1][2]. | ||||||||||||
| Target | IC50: 16 nM (HDAC) | ||||||||||||
| Invitro | Ar-42 (0.125-1 μM; 24 h) 抑制 P815、C2 和 BR 细胞生长的中位 IC50 分别为 0.65、0.30 和 0.23 μM[3]。Ar-42 (0.5 μM; 24 h) 诱导 P815 细胞在 G1/G2 细胞周期阻滞[3]。Ar-42 (0.13-1 μM; 24 h) 诱导 P815, C2, BR 细胞凋亡[3]。Ar-42 (0.5-3 μM; 24 h) 诱导组蛋白 H3、H4 和 α-微管蛋白的超乙酰化[3]。 Cell Proliferation Assay[3] Cell Line: | ||||||||||||
| In Vivo | AR-42 (10mg /kg;尾静脉注射;每周2次，连续3周)显著抑制肿瘤生长[4]。 Animal Model: | ||||||||||||
| Name | AR-42 | ||||||||||||
| CAS | 935881-37-1 | ||||||||||||
| Formula | C18H20N2O3 | ||||||||||||
| Molar Mass | 312.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lu YS, Chou CH, Tzen KY, Gao M, ChLu YS, et al. 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.eng 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. [2]. Lu Q, et al. Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5. [3]. 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. [4]. Zhang M, et al. AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition. Oncotarget. 2016 Apr 19;7(16):22285-94. |