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C0621

CI−994

Name: CI&#8722;994
Brand: SIGMA

≥98% (HPLC), HDAC Inhibitor, powder

Synonym(s):

4-Acetylamino-N-(2′-aminophenyl)benzamide, Acetyldinaline, Tacedinaline

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₁₅N₃O₂

CAS Number:

112522-64-2

Molecular Weight:

269.30

UNSPSC Code:

12352200

PubChem Substance ID:

329774808

NACRES:

NA.77

MDL number:

MFCD00866266

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

CI−994, ≥98% (HPLC), powder

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

off-white

solubility

DMSO: >10 mg/mL

storage temp.

room temp

SMILES string

CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N

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)

InChI key

VAZAPHZUAVEOMC-UHFFFAOYSA-N

Gene Information

human ... HDAC1(3065), HDAC10(83933), HDAC11(79885), HDAC2(3066), HDAC3(8841), HDAC4(9759), HDAC5(10014), HDAC6(10013), HDAC7(51564), HDAC8(55869), HDAC9(9734)

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

Application

CI-994 has been used:

as an histone deacetylase (HDAC) inhibitor to treat SUM229 and DT22 cells to study its effects
as an HDAC inhibitor for screening in SPEL cells
to study its effects on human myeloid and erythroid progenitors

Biochem/physiol Actions

CI-994 is the acetylated derivative form of the original compound Dinaline (PD 104 208). It is an oral cytostatic drug with impressive differential activity against leukemic cells & normal stem-cells. It is used for combination therapy for selected tumors including non-small cell lung, pancreatic, breast, and colorectal cancers. It acts as a histone deacetylase inhibitor. CI-994 blocks cells in the G1-S phase of the cell cycle. The 16 kDa phosphoprotein is confined to the nuclear compartment. Loss of the 16-kDa nuclear phosphoprotein appears to be a direct effect of CI-994 treatment and that the inhibition of this phosphoprotein may play a critical role in the mechanism of action of CI-994.

Orally available HDAC Inhibitor; CI-994 blocks cells in the G1-S phase of the cell cycle.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

pictograms

GHS07

signalword

Warning

hcodes

H319

pcodes

P264 - P280 - P305 + P351 + P338 - P337 + P313

Hazard Classifications

Eye Irrit. 2

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

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The potential role of histone deacetylase inhibitors in the treatment of non-small-cell lung cancer.

Cesare Gridelli et al.

Critical reviews in oncology/hematology, 68(1), 29-36 (2008-04-22)

Non-small-cell lung cancer (NSCLC) arises from a complex series of genetic and epigenetic changes leading to uncontrolled cell growth and metastases. The exponential growth in the level of research about the histone deacetylase (HDAC) enzymes, responsible for deacetylating core nucleosomal

Class I histone deacetylase (HDAC) inhibitor CI-994 promotes functional recovery following spinal cord injury.

Suxiang Zhang et al.

Cell death & disease, 9(5), 460-460 (2018-04-28)

Spinal cord injury (SCI) induces severe and long-lasting neurological disability. Accumulating evidence has suggested that histone deacetylase (HDAC) inhibitors exert neuroprotective effects against various insults and deficits in the central nervous system. In the present study, we assessed the effect

Chronic oral administration of CI-994: a phase 1 study.

S Prakash et al.

Investigational new drugs, 19(1), 1-11 (2001-04-09)

CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts. While cytotoxic in the Brown Norway (BN) rat leukemia model, growth inhibition in other murine and human tumor xenografts

Establishing and characterizing a new primary effusion lymphoma cell line harboring Kaposi?s sarcoma-associated herpesvirus

Osawa M, et al.

Infectious Agents and Cancer, 11(1), 37-37 (2016)

Preclinical antitumor activity of CI-994.

P M LoRusso et al.

Investigational new drugs, 14(4), 349-356 (1996-01-01)

CI-994 [aka: acetyldinaline; PD 123654; 4-acetylamino-N-(2'aminophenyl)-benzamide] (Figure 1) is a novel antitumor agent with a unique mechanism of action. It is the acetylated metabolite of dinaline, a compound previously identified as having cytotoxic and cytostatic activity against several murine and

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Discover Bioactive Small Molecules for Gene Regulation

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

Global Trade Item Number

SKU	GTIN
C0621-25MG	04061833217863
C0621-5MG	04061833217870

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