MPT0E028 | HDAC inhibitor | Probechem Biochemicals

Chemical Structure : MPT0E028

CAS No.: 1338320-94-7

MPT0E028 (Imofinostat, MPT0 E028)

Catalog No.: PC-35302Not For Human Use, Lab Use Only.

Imofinostat (MPT0E028) is a potent HDAC inhibitor with IC50 of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively, inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA.

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Biological Activity

Imofinostat (MPT0E028) is a potent HDAC inhibitor with IC50 of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively, inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA.
MPT0E028 inhibits class I HDAC1, HDAC2, and class Iib HDAC6 with IC50 of 53, 106, and 29.5 nM, respectively, weakly inhibits HDAC8 (IC50=2.5 uM), but not for HDAC4 (IC50>10 uM).
MPT0E028 inhibits the growth of HCT116 and MDA-MB-231 cells with IC50 of 0.09 and 0.19 uM.
MPT0E028 inhibits HCT116 tumor xenograft in vivo without significant adverse effects, shows stronger anti-cancer efficacy than SAHA.

Physicochemical Properties

M.Wt	344.385
Formula	C17H16N2O4S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide

References

1. Huang HL, et al. PLoS One. 2012;7(8):e43645.

2. Chen MC, et al. Cell Death Dis. 2013 Sep 19;4:e810.

3. Chen CH, et al. Clin Cancer Res. 2014 Mar 1;20(5):1274-1287.

4. Huang HL, et al. Oncotarget. 2015 Mar 10;6(7):4976-91.

MPT0E028 (Imofinostat, MPT0 E028)

Biological Activity

Physicochemical Properties

References

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