tet1

Bobcat339 is a novel cytosine-based TET enzyme inhibitor (IC50s: 33 73 uM for TET1 2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a.

UC-514321 directly targets STAT3 5 and represses TET1 expression. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

TETi76 is an orally active inhibitor from the TET family, demonstrating IC50 values of 1.5, 9.4, and 8.8 μM against TET1, TET2, and TET3, respectively. The compound competitively binds to the active sites of TET enzymes, reducing cytosine hydroxymethylation and restricting clonal growth in mutated TET2 in vitro and in vivo, without affecting the growth of normal hematopoietic progenitor cells. TETi76 is utilized in leukemia research.

OAC1 (BAS 00287861) is a compound activating Octamer-binding transcription factor 4 (Oct4). It enhances the iPSC reprogramming efficiency and accelerates the reprogramming process.

Bobcat339 hydrochloride is a selective 10 11 translocation (TET) dioxygenase inhibitor that inhibits TET1 and TET2.Bobcat339 hydrochloride induces TET3 protein degradation and also stimulates the expression of AGRP, NPY, and VGAT in a TET3-dependent manner in mouse and human neuronal cells. VGAT expression, which can be used to study transient anorexia nervosa.

Succinic acid sodium is an orally active anxiolytic. Succinic acid sodium down-regulates the expression of KCNMB1 (potassium channel subunit β1) and TET1 (10-11 translocation 1). succinic acid sodium inhibits the proliferation of colonic epithelial cells in vivo. Succinic acid sodium can be used to study hypertension in pregnancy.

NSC-311068 is a novel selective inhibitor of TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification, effectively inhibiting cell viability in AML with high expression of TET1.

NSC 370284 is a small molecule that directly binds to and inhibits STAT3 5, significantly and selectively suppresses the viability of AML cells with high level of TET1 expression both in vitro and in vivo.