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Merck

C0621

CI−994

≥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

Key Documents

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Product Name

CI−994, ≥98% (HPLC), powder

SMILES string

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

InChI key

VAZAPHZUAVEOMC-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

powder

color

off-white

solubility

DMSO: >10 mg/mL

storage temp.

room temp

Quality Level

100

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)

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This Item
SML1616SML0638SML1624
CI−994 ≥98% (HPLC), powder

Sigma-Aldrich

C0621

CI−994

ICA-069673 ≥98% (HPLC)

Sigma-Aldrich

SML1616

ICA-069673

S0859 ≥98% (HPLC)

Sigma-Aldrich

SML0638

S0859

JNJ-63533054 ≥98% (HPLC)

Sigma-Aldrich

SML1624

JNJ-63533054

form

powder

form

powder

form

powder

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

room temp

storage temp.

room temp

storage temp.

2-8°C

storage temp.

room temp

solubility

DMSO: >10 mg/mL

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

color

off-white

color

white to beige

color

white to light brown

color

white to beige

Application

CI-994 has been used:
  • as an histone deacetylase (HDAC) inhibitor to treat SUM229 and DT22 cells to study its effects[1]
  • as an HDAC inhibitor for screening in SPEL cells[2]
  • to study its effects on human myeloid and erythroid progenitors[3]

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

Exclamation mark
GHS07

signalword

Warning

hcodes

H319

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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Certificates of Analysis (COA)

Lot/Batch Number
0000208192
0000208192
0000139827
0000139828
0000138977

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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)
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
Ekaterina P Mochalova et al.
Scientific reports, 9(1), 10263-10263 (2019-07-18)
It is known that MuRF-1 and atrogin-1/MAFbx mRNA expression is increased in rat soleus muscle under unloading conditions. We aimed to determine the role of histone deacetylase 1 (HDAC1) in the activation of MuRF-1 and MAFbx expression in rat soleus
S D Undevia et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 15(11), 1705-1711 (2004-11-03)
This study was conducted to determine the toxicity profile, maximum tolerated dose (MTD) and pharmacokinetics of the putative histone deacetylase inhibitor CI-994 in combination with capecitabine. Fifty-four patients were treated according to three different dosing schemes in which the capecitabine
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
View All Related Papers

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