Imofinostat

Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 ​​μM), but no inhibitory effect on HDAC4 (IC50>10 μM) . Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis[1][2][3][14][5][6].

1338320-94-7

ABT-301; MPT0E028; TMU-C-0012

12352005

Akt; Apoptosis; HDAC

Reference compound

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; PI3K/Akt/mTOR

Cancer-Kinase/protease

Cancer; Inflammation/Immunology

https://www.medchemexpress.com/mpt0e028.html

99.40

DMSO : 100 mg/mL (ultrasonic)

O=C(/C=C/C1=CC2=C(C=C1)N(CC2)S(=O)(C3=CC=CC=C3)=O)NO

C17H16N2O4S

344.38

[1]Huang HL, et al. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7 (8) :e43645.|[2]Huang HL, et al. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6 (7) :4976-91.|[3]Chen MC, et al. The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells. Cell Death Dis. 2013 Sep 19;4 (9) :e810. doi: 10.1038/cddis.2013.330. Erratum in: Cell Death Dis. 2024 Jul 9;15 (7) :490. |[4]Yeh LY, et al. A Potent Histone Deacetylase Inhibitor MPT0E028 Mitigates Emphysema Severity via Components of the Hippo Signaling Pathway in an Emphysematous Mouse Model. Front Med (Lausanne) . 2022 May 18;9:794025. |[5]Liu CH, et al. MPT0E028, a novel pan-HDAC inhibitor, prevents pulmonary fibrosis through inhibition of TGF-β-induced CTGF expression in human lung fibroblasts: Involvement of MKP-1 activation. Eur J Pharmacol. 2024 Aug 15;977:176711.|[6]Chao MW, et al. Combination treatment strategy for pancreatic cancer involving the novel HDAC inhibitor MPT0E028 with a MEK inhibitor beyond K-Ras status. Clin Epigenetics. 2019 May 29;11 (1) :85.

Room Temperature

4°C (Powder, sealed storage, away from moisture and light)

Reference compound1

Phase 1