MPT0E028

Names

[ Name ]:
MPT0E028

[Synonym ]:
3-(1-(Benzenesulfonyl)-2,3-dihydro-1H-indol-5-yl)-N-hydroxyacrylamide
2-Propenamide,3-(2,3-dihydro-1-(phenylsulfonyl)-1H-indol-5-yl)-N-hydroxy
UNII-T65L58FI65

Biological Activity

[Description]:

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[1]. MPT0E028 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. MPT0E028 has good anticancer activity[2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

[Target]

HDAC1:53.0 nM (IC50)

HDAC2:106.2 nM (IC50)

HDAC6:29.5 nM (IC50)

HDAC8:2532.6 nM (IC50)

Akt

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₆N₂O₄S

[ Molecular Weight ]:
344.38500

[ Exact Mass ]:
344.08300

[ PSA ]:
98.58000

[ LogP ]:
3.94270

Related Compounds

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