SB939 is a novel potent and orally active histone deacetylase inhibitor with an IC50 of 52 nM for HDAC1 and a GI50 of 0.56 µM for Colo205. Its IC50 for HCT-116 colon cancer cell line and HL-60 acute myeloid leukemia cell line is 0.48 ¦ÌM and 70 nM, respectively. In vitro, SB939 inhibits class I, II, and IV HDACs, with no effects on other zinc binding enzymes, and shows significant antiproliferative activity against a wide variety of tumor cell lines. It has very favorable pharmacokinetic properties after oral dosing in mice, with >4-fold increased bioavailability and 3.3-fold increased half-life over suberoylanilide hydroxamic acid (SAHA). In contrast to SAHA, SB939 accumulates in tumor tissue and induces a sustained inhibition of histone acetylation in tumor tissue.

June 21, 2017

prudect name : SB939 is a novel potent and orally active histone deacetylase inhibitor with an IC50 of 52 nM for HDAC1 and a GI50 of 0.56 µM for Colo205. Its IC50 for HCT-116 colon cancer cell line and HL-60 acute myeloid leukemia cell line is 0.48 ¦ÌM and 70 nM, respectively. In vitro, SB939 inhibits class I, II, and IV HDACs, with no effects on other zinc binding enzymes, and shows significant antiproliferative activity against a wide variety of tumor cell lines. It has very favorable pharmacokinetic properties after oral dosing in mice, with >4-fold increased bioavailability and 3.3-fold increased half-life over suberoylanilide hydroxamic acid (SAHA). In contrast to SAHA, SB939 accumulates in tumor tissue and induces a sustained inhibition of histone acetylation in tumor tissue.
SB939 (Pracinostat)

Synonyms: SB939 (Pracinostat)CAS NO: 929016-96-6Molecular Formula: C₂₀H₃₀N₄O₂Molecular Weight: 358.48Purity: 98% minSolubility: In DMSOStorage: -20°C

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