TET Protein Inhibitor

Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.

Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.

TETi76 is an orally active TET family inhibitor with IC₅₀ values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.

NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.

NSC-311068 is TET1 inhibitor. NSC-311068 selectively suppress TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification. NSC-311068 represses the level of TET1 expression and the global 5hmC level. NSC-311068 effectively inhibits cell viability in AML cells with high expression of TET1.

UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

Succinic acid sodium is a potent and orally active anxiolytic agent. Succinic acid sodium shows inhibitory effects on colonic epithelial cell proliferation in vivo. Succinic acid sodium can down-regulate the expression of KCNMB1 (potassium channel subunit β1) and TET1 (ten?eleven translocation 1). Succinic acid sodium can be used for gestational hypertension research.