| Chemical Properties | Back Directory | [Boiling point ]
491.4±55.0 °C(predicted) | [density ]
1.397±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
0.25±0.10(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice[1][2]. | [in vivo]
SE-7552 (30 mg/kg; a single oral dose) increases the levels of acetylated α-tubulin for over 24 hours in mice. SE-7552 has no effect on the acetylation of H3 (a biomarker for inhibition of Class I HDACs)[1].
SE-7552 (10 mg/kg; orally; daily) combinated with Pomalidomide (HY-10984; 1 mg/kg; IP daily) significantly delays tumor growth in comparison to Pomalidomide alone, as well as enhanced the survival of the mice with human H929 MM cells[1].
SE-7552 demonstrated superior PK, with a maximum exposure of 597 ng/ml and a half-life of 7.2 hours after a single oral dose of 5 mg/kg in the mouse[1].
| [IC 50]
HDAC6: 33 nM (IC50) | [References]
[1] Jason A Holt, et al. SE-7552, a Highly Selective, Non-Hydroxamate Inhibitor of Histone Deacetylase-6 Blocks Multiple Myeloma Growth In Vivo. Blood (2018) 132 (Supplement 1): 3215.
[2] Beate K?nig, et al. 2-(Difluoromethyl)-1,3,4-oxadiazoles: The Future of Selective Histone Deacetylase 6 Modulation? ACS Pharmacol. Transl. Sci. 2024, February 20. |
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