bs-60186C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 269.3

Formula: C15 H15 N3 O2

CAS Number: 112522-64-2

InChi Key: VAZAPHZUAVEOMC-UHFFFAOYSA-N

InChi: InChI=1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20)

Smiles: CC(=O)NC1C=CC(=CC=1)C(=O)NC1C=CC=CC=1N

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

CI994 is a potent, selective and orally active histone deacetylase (HDAC) inhibitor. It inhibits HDAC1 (IC50 ~0.57 µM), HDAC2 (IC50 ~0.90 µM) and HDAC3 (IC50 ~1.2 µM). It does not inhibit HDAC6 and HDAC8 (IC50 >100 µM). CI994 mediates G1 cell cycle arrest, inhibits proliferation, and induces apoptosis in tumor cell lines. It has also demonstrated antitumor activity in several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP. Currently CI994 is in phase III clinical trials for lung cancer. In recent publication CI994 could also epigenetically prime the hippocampal transcriptome for reinstated neuroplasticity and lead to increased neuroplasticity during memory extinction. This suggests applying HDACis during memory reconsolidation might constitute a treatment option for remote traumata.