CI994 (Tacedinaline) --- HDAC Inhibitor


Catalog No. size PriceQuantity
M60186-2S 2 mg solid $79
M60186-10S 10mg solid $320

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.

Product information

CAS Number: 112522-64-2

Molecular Weight: 269.30

Formula: C15H15N3O2

Chemical Name: 4-acetamido-N-(2-aminophenyl)benzamide

Smiles: CC(=O)NC1C=CC(=CC=1)C(=O)NC1=CC=CC=C1N

InChiKey: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

CI994 was used at 2.5-10 µM in vitro and cellular assays.

In Vivo:

CI994 was administered to mice via oral gavage (PO) or intraperitoneal injection (IP) at 5-35 mg/kg once per day.

References:

  1. Kraker AJ, et al. Modulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinoma. (2003) Mol Cancer Ther. 2(4):401-8.
  2. Loprevite M, et al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. (2005) Oncol Res. 15(1):39-48.

Products are for research use only. Not for human use.


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